Lamivudine
别名: GR109714X, BCH-189 中文名称：拉米夫定, 拉美呋定, 拉米呋啶
Lamivudine是一种有效的核苷类似物逆转录酶抑制剂，用于治疗慢性乙肝和艾滋病。它主要是通过阻滞HIV逆转录酶和乙肝病毒聚合酶发挥其作用。
Lamivudine Chemical Structure
CAS: 134678-17-4
客户使用Selleck的Lamivudine发表文献16篇
客户使用该产品的1个实验数据
产品质控
批次：
纯度：
99.94%
99.94
相关信号通路图
Reverse Transcriptase抑制剂选择性比较
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| PBMC | Function assay | 300 mg | 7 days | Cmax in HIV-infected human assessed as Lamivudine monophosphate level in PBMC at 300 mg QD for 7 days measured per 10'6 cells in presence of zidovudine, Cmax=0.0000008μM | 17664328 |
| PBMC | Function assay | 300 mg | 7 days | Cmax in HIV-infected human assessed as Lamivudine diphosphate level in PBMC at 300 mg QD for 7 days measured per 10'6 cells in presence of zidovudine, Cmax=0.0000044μM | 17664328 |
| PBMC | Function assay | 300 mg | 7 days | Cmax in HIV-infected human assessed as Lamivudine triphosphate level in PBMC at 300 mg QD for 7 days measured per 10'6 cells in presence of zidovudine, Cmax=0.0000048μM | 17664328 |
| HepG2(2.2.15) | Antiviral assay | 13 uM | 72 hrs | Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as decrease in intracellular viral DNA level at 13 uM after 72 hrs by RT-PCR analysis | 20176893 |
| HepG2(2.2.15) | Function assay | 0.75 to 3 uM | 72 hrs | Decrease in HBV viral DNA replication in human HepG2(2.2.15) cells at 0.75 to 3 uM after 72 hrs by real-time PCR analysis, IC50=7.63μM | 25461891 |
| U87 | Antiviral assay | 10 uM | 4 days | Antiviral activity against HIV-1 NL4-3 infected in human U87 cells expressing CD4.CXCR4 assessed as inhibition of p24 production at 10 uM measured after 4 days by p24 ELISA | 27091070 |
| U87 | Antiviral assay | 100 uM | 4 days | Antiviral activity against HIV-1 NL4-3 infected in human U87 cells expressing CD4.CXCR4 assessed as inhibition of p24 production at 100 uM measured after 4 days by p24 ELISA | 27091070 |
| HepG2.2.15 | Function assay | 4 uM | 6 days | Inhibition of capsid protein in Hepatitis B virus infected in human HepG2.2.15 cells assessed as reduction in viral DNA level at 4 uM supplemented with fresh medium containing compound every 2 days and measured after 6 days by RT-PCR analysis, IC50<0.1μM | 31091479 |
| MDCK2 | Function assay | 10 uM | Inhibition of human MRP2 expressed in MDCK2 cells assessed as increase in intracellular CMF fluorescence at 10 uM by CMFDA assay | 17172311 | |
| MDCK2 | Function assay | 10 uM | Inhibition of human MRP3 expressed in MDCK2 cells assessed as increase in intracellular CMF fluorescence at 10 uM by CMFDA assay | 17172311 | |
| MDCK2 | Function assay | 10 uM | Inhibition of human MRP1 expressed in MDCK2 cells assessed as increase in intracellular CMF fluorescence at 10 uM by CMFDA assay | 17172311 | |
| CEM-SS | Antiviral assay | 6 days | Antiviral activity against HIV1 3B infected in human CEM-SS cells assessed as inhibition of virus-induced cytopathic effect after 6 days by MTS assay, ED50=0.36μM | 15217281 | |
| HOG.R5 | Antiviral assay | 4 days | Antiviral activity against HIV1 3B infected in human HOG.R5 cells after 4 days, IC50=1.2μM | 15217281 | |
| Huh7 | Antiviral assay | 5 days | Antiviral activity against HBV genotype D with reverse transcriptase L80I mutation in human Huh7 cells assessed as inhibition of viral replication after 5 days, EC50=0.03μM | 17438047 | |
| Huh7 | Antiviral assay | 5 days | Antiviral activity against HBeAg-deficient HBV genotype D with precore G1896A mutation and reverse transcriptase L80I mutation in human Huh7 cells assessed as inhibition of viral replication after 5 days, EC50=0.03μM | 17438047 | |
| Huh7 | Antiviral assay | 5 days | Antiviral activity against HBV genotype D in human Huh7 cells assessed as inhibition of viral replication after 5 days, EC50=0.41μM | 17438047 | |
| Huh7 | Antiviral assay | 5 days | Antiviral activity against HBeAg-deficient HBV genotype D with precore G1896A mutation in human Huh7 cells assessed as inhibition of viral replication after 5 days, EC50=0.46μM | 17438047 | |
| HepG2.2.15 | Function assay | 8 days | Inhibition of cytoplasmic HBV DNA synthesis in HepG2.2.15 cells after 8 days, IC50=0.38μM | 17499889 | |
| MAGIC-5A | Antiviral assay | 40 hrs | Antiviral activity against wild type HIV1 NL4-3 produced from full length pR9deltaApa infected in human MAGIC-5A cells assessed as inhibition of Lac+ foci expression after 40 hrs, EC50=0.88μM | 17967913 | |
| MAGIC-5A | Antiviral assay | 40 hrs | Antiviral activity against wild type HIV2 ROD produced from full length pROD9 infected in human MAGIC-5A cells assessed as inhibition of Lac+ foci expression after 40 hrs, EC50=2μM | 17967913 | |
| MAGIC-5A | Antiviral assay | 40 hrs | Antiviral activity against multinucleoside-resistant HIV1 NL4-3 harboring A62V, V75I, F77L, F116Y, Q151M mutation in viral reverse transcriptase infected in human MAGIC-5A cells assessed as inhibition of Lac+ foci expression after 40 hrs, EC50=3.7μM | 17967913 | |
| PBMC | Antiviral assay | 1 hr | Antiviral activity against HIV1 subtype B-ASM 044 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA, EC50=0.04μM | 18316521 | |
| MT2 | Antiviral assay | 5 days | Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA, EC50=0.04μM | 18316521 | |
| MT2 | Antiviral assay | 5 days | Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA, EC50=0.063μM | 18316521 | |
| MT2 | Antiviral assay | 5 days | Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA, EC50=0.086μM | 18316521 | |
| MT2 | Antiviral assay | 1 hr | Antiviral activity against HIV1 subtype B-RF infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA, EC50=0.105μM | 18316521 | |
| MT2 | Antiviral assay | 1 hr | Antiviral activity against HIV1 subtype B-NL4-3 infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA, EC50=0.171μM | 18316521 | |
| MT2 | Antiviral assay | 1 hr | Antiviral activity against HIV1 subtype B-LAI infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA, EC50=0.182μM | 18316521 | |
| MT2 | Antiviral assay | 1 hr | Antiviral activity against HIV1 subtype B-SF-2 infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA, EC50=0.183μM | 18316521 | |
| MT2 | Antiviral assay | 1 hr | Antiviral activity against HIV1 subtype B-HXB2 infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA, EC50=0.202μM | 18316521 | |
| MT2 | Antiviral assay | 5 days | Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay, EC50=0.219μM | 18316521 | |
| MT2 | Antiviral assay | 5 days | Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA, EC50=0.372μM | 18316521 | |
| MT2 | Antiviral assay | 5 days | Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA, EC50=0.462μM | 18316521 | |
| MT2 | Antiviral assay | 5 days | Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay, EC50=0.554μM | 18316521 | |
| MT2 | Antiviral assay | 5 days | Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA, EC50=0.667μM | 18316521 | |
| PBMC | Antiviral assay | 1 hr | Antiviral activity against HIV1 subtype B-93US143 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA, EC50=0.85μM | 18316521 | |
| MT2 | Antiviral assay | 5 days | Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay, EC50=0.927μM | 18316521 | |
| MT2 | Antiviral assay | 5 days | Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay, EC50=0.969μM | 18316521 | |
| MT2 | Antiviral assay | 5 days | Antiviral activity against pseudotype HIV1 NL-RLuc infected in human MT2 cells measured on day 5 postinfection by luciferase reporter gene assay, EC50=1.14μM | 18316521 | |
| MT2 | Antiviral assay | 5 days | Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay, EC50=1.259μM | 18316521 | |
| MT2 | Antiviral assay | 5 days | Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay, EC50=1.683μM | 18316521 | |
| MT2 | Antiviral assay | 5 days | Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA, EC50=1.985μM | 18316521 | |
| MT2 | Antiviral assay | 5 days | Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay, EC50=2.445μM | 18316521 | |
| MT2 | Antiviral assay | 5 days | Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA, EC50=2.47μM | 18316521 | |
| MT2 | Antiviral assay | 5 days | Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay, EC50=3.247μM | 18316521 | |
| HepG2(2.2.15) | Antiviral assay | 24 hrs | Antiviral activity against HBV in human HepG2(2.2.15) cells assessed as extracellular HBV virion DNA level after 24 hrs, EC50=0.048μM | 19072694 | |
| HepG2(2.2.15) | Antiviral assay | 24 hrs | Antiviral activity against HBV in human HepG2(2.2.15) cells assessed as replication intermediates after 24 hrs, EC50=0.15μM | 19072694 | |
| Huh7 | Antiviral assay | 4 days | Antiviral activity against lamivudine-resistant wild type HBV in human Huh7 cells after 4 days by intracellular HBV DNA replication assay, EC50=0.2μM | 19072694 | |
| Huh7 | Antiviral assay | 4 days | Antiviral activity against lamivudine-resistant HBV reverse transcriptase 236T mutant in human Huh7 cells after 4 days by intracellular HBV DNA replication assay, EC50=0.3μM | 19072694 | |
| Huh7 | Antiviral assay | 4 days | Antiviral activity against adefovir-resistant wild type HBV in human Huh7 cells after 4 days by intracellular HBV DNA replication assay, EC50=1.3μM | 19072694 | |
| Huh7 | Antiviral assay | 4 days | Antiviral activity against adefovir-resistant HBV reverse transcriptase M204V mutant in human Huh7 cells after 4 days by intracellular HBV DNA replication assay, EC50=1.5μM | 19072694 | |
| Huh7 | Antiviral assay | 4 days | Antiviral activity against adefovir-resistant HBV reverse transcriptase L180M mutant in human Huh7 cells after 4 days by intracellular HBV DNA replication assay, EC50=1.6μM | 19072694 | |
| Huh7 | Antiviral assay | 4 days | Antiviral activity against adefovir-resistant HBV reverse transcriptase LM/reverse transcriptase MV double mutant in human Huh7 cells after 4 days by intracellular HBV DNA replication assay, EC50=1.6μM | 19072694 | |
| Huh7 | Antiviral assay | 4 days | Antiviral activity against adefovir-resistant HBV reverse transcriptase M204I mutant in human Huh7 cells after 4 days by intracellular HBV DNA replication assay, EC50=1.8μM | 19072694 | |
| Huh7 | Antiviral assay | 4 days | Antiviral activity against adefovir-resistant HBV reverse transcriptase 236T mutant in human Huh7 cells after 4 days by intracellular HBV DNA replication assay, EC50=7.7μM | 19072694 | |
| Huh7 | Antiviral assay | 4 days | Antiviral activity against lamivudine-resistant HBV reverse transcriptase L180M mutant in human Huh7 cells after 4 days by intracellular HBV DNA replication assay, EC50=10μM | 19072694 | |
| HuH7 | Antiviral assay | 24 hrs | Antiviral activity against wild type HBV infected in human HuH7 cells assessed as decrease in viral transient transfection after 24 hrs, EC50=0.2μM | 19398648 | |
| HuH7 | Antiviral assay | 24 hrs | Antiviral activity against HBV harboring RNA polymerase N236T mutant gene infected in human HuH7 cells assessed as decrease in viral transient transfection after 24 hrs, EC50=0.3μM | 19398648 | |
| HuH7 | Antiviral assay | 24 hrs | Antiviral activity against HBV harboring RNA polymerase N236T mutant gene infected in human HuH7 cells assessed as decrease in viral transient transfection after 24 hrs, EC90=1.5μM | 19398648 | |
| HuH7 | Antiviral assay | 24 hrs | Antiviral activity against wild type HBV infected in human HuH7 cells assessed as decrease in viral transient transfection after 24 hrs, EC90=3μM | 19398648 | |
| HuH7 | Antiviral assay | 24 hrs | Antiviral activity against HBV harboring RNA polymerase L180M mutant gene infected in human HuH7 cells assessed as decrease in viral transient transfection after 24 hrs, EC50=16μM | 19398648 | |
| HuH7 | Antiviral assay | 24 hrs | Antiviral activity against HBV harboring RNA polymerase L180M mutant gene infected in human HuH7 cells assessed as decrease in viral transient transfection after 24 hrs, EC90=41μM | 19398648 | |
| TZM-bl | Antiviral assay | 72 hrs | Antiviral activity against HIV1 pNL4-3 harboring Reverse transcriptase P119S mutant gene infected in TZM-bl cells after 72 hrs by luciferase assay, EC50=0.47μM | 19704131 | |
| TZM-bl | Antiviral assay | 72 hrs | Antiviral activity against HIV1 pNL4-3 harboring Reverse transcriptase T165A mutant gene infected in TZM-bl cells after 72 hrs by luciferase assay, EC50=1.08μM | 19704131 | |
| TZM-bl | Antiviral assay | 72 hrs | Antiviral activity against HIV1 pNL4-3 harboring Reverse transcriptase P119S/T165A mutant gene infected in TZM-bl cells after 72 hrs by luciferase assay, EC50=2.1μM | 19704131 | |
| 1.3ES2 | Antiviral assay | 6 days | Antiviral activity against Hepatitis B virus ayw in human 1.3ES2 cells stably transfected with 1.3 fold wild type HBV ayw strain genome cells assessed as reduction of viral DNA level after 6 days by RT-PCR | 20061158 | |
| HepG2.2.15 | Antiviral assay | 9 days | Antiviral activity against wild type HBV infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization, EC50=0.2μM | 20117930 | |
| HepG2.2.15 | Antiviral assay | 9 days | Antiviral activity against ADV-resistant HBV N236T mutation infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization, EC50=0.2μM | 20117930 | |
| HepG2.2.15 | Antiviral assay | 9 days | Antiviral activity against wild type HBV infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization, EC90=0.7μM | 20117930 | |
| HepG2.2.15 | Antiviral assay | 9 days | Antiviral activity against ADV-resistant HBV N236T mutation infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization, EC90=0.8μM | 20117930 | |
| HepG2.2.15 | Antiviral assay | 9 days | Antiviral activity against 3TC-resistant HBV with polymerase L180M mutation infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization, EC50=5.3μM | 20117930 | |
| HepG2.2.15 | Antiviral assay | 9 days | Antiviral activity against 3TC-resistant HBV with polymerase L180M mutation infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization, EC90=20μM | 20117930 | |
| HEK293 | Antiviral assay | 72 hrs | Antiviral activity against HIV1 subtype D isolate 8 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs, EC50=3.25μM | 20308377 | |
| HEK293 | Antiviral assay | 72 hrs | Antiviral activity against HIV1 subtype A isolate 1 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs, EC50=3.54μM | 20308377 | |
| HEK293 | Antiviral assay | 72 hrs | Antiviral activity against HIV1 subtype C isolate 6 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs, EC50=3.9μM | 20308377 | |
| HEK293 | Antiviral assay | 72 hrs | Antiviral activity against HIV1 subtype C isolate 7 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs, EC50=4.06μM | 20308377 | |
| HEK293 | Antiviral assay | 72 hrs | Antiviral activity against HIV1 subtype BF isolate 5 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs, EC50=4.24μM | 20308377 | |
| HEK293 | Antiviral assay | 72 hrs | Antiviral activity against HIV1 subtype A isolate 2 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs, EC50=4.48μM | 20308377 | |
| HEK293 | Antiviral assay | 72 hrs | Antiviral activity against HIV1 NL4-3 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs, EC50=4.68μM | 20308377 | |
| HEK293 | Antiviral assay | 72 hrs | Antiviral activity against HIV1 subtype B isolate 3 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs, EC50=4.78μM | 20308377 | |
| HEK293 | Antiviral assay | 72 hrs | Antiviral activity against HIV1 subtype B isolate 4 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs, EC50=5.43μM | 20308377 | |
| HEK293 | Antiviral assay | 72 hrs | Antiviral activity against HIV1 expressing reverse transcriptase K103N/Y181C/G190A mutant infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs, EC50=7.16μM | 20308377 | |
| HepG2(2.2.15) | Antiviral assay | 8 days | Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as inhibition of viral cytoplasmic DNA synthesis after 8 days by RT-PCR analysis, IC50=0.16μM | 20639110 | |
| HepG2(2.2.15) | Cytotoxicity assay | 8 days | Cytotoxicity against human HepG2(2.2.15) cells after 8 days by MTT assay, CC50=5μM | 20639110 | |
| MT2 | Antiviral assay | 2 to 3 days | Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect measured after 2 to 3 days by PCR, EC50=0.8μM | 21115794 | |
| Huh7 | Antiviral assay | 1 day | Antiviral activity against Hepatitis B virus infected in human Huh7 cells assessed as reduction in viral DNA after 1 day by Southern blotting, EC50=0.1μM | 21333535 | |
| HuH7 | Cytotoxicity assay | 4 days | Cytotoxicity against human HuH7 cells after 4 days by neutral red dye uptake assay, CC50=0.1μM | 21333535 | |
| HepG2(2.2.15) | Antiviral assay | 4 days | Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as inhibition of viral DNA replication after 4 days by RT-PCR analysis, IC50=0.33μM | 21524588 | |
| HepG2(2.2.15) | Antiviral assay | 9 days | Antiviral activity against wild type Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as inhibition of virus replication treated daily for 9 days by quantitative blot hybridization method, EC50=0.2μM | 21930377 | |
| HepG2(2.2.15) | Antiviral assay | 9 days | Antiviral activity against adefovir-resistant Hepatitis B virus harboring reverse transcriptase N236T mutant infected in human HepG2(2.2.15) cells assessed as inhibition of virus replication treated daily for 9 days by quantitative blot hybridization meth, EC50=0.2μM | 21930377 | |
| HepG2(2.2.15) | Antiviral assay | 9 days | Antiviral activity against wild type Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as reduction of infectious virus titer treated daily for 9 days by quantitative Southern blot hybridization assay, EC90=0.6μM | 21930377 | |
| HepG2(2.2.15) | Antiviral assay | 9 days | Antiviral activity against adefovir-resistant Hepatitis B virus harboring reverse transcriptase N236T mutant infected in human HepG2(2.2.15) cells assessed as reduction of infectious virus titer treated daily for 9 days by quantitative Southern blot hybri, EC90=0.9μM | 21930377 | |
| HepG2(2.2.15) | Antiviral assay | 9 days | Antiviral activity against lamivudine-resistant Hepatitis B virus harboring reverse transcriptase L180M mutant infected in human HepG2(2.2.15) cells assessed as inhibition of virus replication treated daily for 9 days by quantitative blot hybridization me, EC50=1.5μM | 21930377 | |
| HepG2(2.2.15) | Antiviral assay | 9 days | Antiviral activity against lamivudine-resistant Hepatitis B virus harboring reverse transcriptase L180M mutant infected in human HepG2(2.2.15) cells assessed as reduction of infectious virus titer treated daily for 9 days by quantitative Southern blot hyb, EC90=22μM | 21930377 | |
| HeLa P4/R5 | Antiviral assay | 2 hrs | Antiviral activity against HIV1 BaL infected in HeLa P4/R5 cells assessed as reduction of viral infection incubated for 2 hrs followed by incubated in drug-free medium for 46 hrs by single round infection beta-galactosidase reporter gene assay, EC50=11.3μM | 22352809 | |
| HeLa P4/R5 | Antiviral assay | 2 hrs | Antiviral activity against HIV1 3B infected in HeLa P4/R5 cells assessed as reduction of viral infection incubated for 2 hrs followed by incubated in drug-free medium for 46 hrs by single round infection beta-galactosidase reporter gene assay, EC50=32.7μM | 22352809 | |
| HeLa P4/R5 | Antiviral assay | 2 hrs | Antiviral activity against HIV1 BaL assessed as inhibition of infection in HeLa P4/R5 cells expressing CD4 receptor and beta-gal incubated for 2 hrs followed by compound-wash out measured after 46 hrs by single round infection MAGI assay, EC50=11.4μM | 22533850 | |
| HeLa P4/R5 | Antiviral assay | 2 hrs | Antiviral activity against HIV1 3B assessed as inhibition of infection in HeLa P4/R5 cells expressing CD4 receptor and beta-gal incubated for 2 hrs followed by compound-wash out measured after 46 hrs by single round infection MAGI assay, EC50=32.7μM | 22533850 | |
| CEM-SS | Antiviral assay | 6 days | Antiviral activity against HIV-1 subtype 3B infected in CEM-SS cells assessed as inhibition of viral replication after 6 days by XTT assay, EC50=0.2μM | 22858097 | |
| MT4 | Antiviral assay | 5 days | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against viral-induced cytotoxicity after 5 days by MTT assay, EC50=1.8μM | 24119448 | |
| MT4 | Antiviral assay | 5 days | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as protection against viral-induced cytotoxicity after 5 days by MTT assay, EC50=5.9μM | 24119448 | |
| CEM | Antiviral assay | 4 days | Antiviral activity against HIV1 3B infected in human CEM cells assessed as virus-induced giant cell formation after 4 days by microscopic analysis, EC50=0.099μM | 24177359 | |
| CEM | Antiviral assay | 4 days | Antiviral activity against HIV2 ROD infected in human CEM cells assessed as virus-induced giant cell formation after 4 days by microscopic analysis, EC50=0.18μM | 24177359 | |
| MT4 | Antiviral assay | 5 days | Antiviral activity against Human immunodeficiency virus 1 3b infected in human MT4 cells assessed as inhibition of virus replication after 5 days by MTT assay, IC50=3.9μM | 24926807 | |
| MT4 | Antiviral assay | 5 days | Antiviral activity against Human immunodeficiency virus type 2 ROD infected in human MT4 cells assessed as inhibition of virus replication after 5 days by MTT assay, IC50=15.5μM | 24926807 | |
| MT4 | Antiviral assay | 5 days | Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay, IC50=3.89μM | 24952305 | |
| MT4 | Antiviral assay | 5 days | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay, IC50=15.53μM | 24952305 | |
| MT4 | Antiviral assay | 5 days | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay, EC50=2.22μM | 25240095 | |
| MT4 | Antiviral assay | 5 days | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay, EC50=8.81μM | 25240095 | |
| MT4 | Antiviral assay | 5 days | Antiviral activity against wild type HIV-1 3B infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay, EC50=2.24μM | 25537532 | |
| MT4 | Antiviral assay | 5 days | Antiviral activity against wild type HIV-2 ROD infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay, EC50=8.79μM | 25537532 | |
| MT4 | Antiviral assay | 5 days | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay, EC50=2.239μM | 25626145 | |
| MT4 | Antiviral assay | 5 days | Antiviral activity against HIV1 3B infected infected in human MT4 cells assessed as protection against virus-induced cytotoxicity after 5 days by MTT assay, EC50=0.89μM | 25682562 | |
| MT4 | Antiviral assay | 5 days | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as protection against virus-induced cytotoxicity after 5 days by MTT assay, EC50=3.56μM | 25682562 | |
| MT4 | Antiviral assay | 5 days | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay, EC50=2.2μM | 25707013 | |
| MT4 | Antiviral assay | 5 days | Antiviral activity against HIV1-3B infected in human MT4 cells assessed as inhibition of virus induced cell death measured after 5 days of infection by MTT assay, EC50=3.9μM | 25946116 | |
| MT4 | Antiviral assay | 5 days | Antiviral activity against HIV2-ROD infected in human MT4 cells assessed as inhibition of virus induced cell death measured after 5 days of infection by MTT assay, EC50=15.5μM | 25946116 | |
| HepG22.2.15 | Antiviral assay | 3 days | Antiviral activity against HBV infected in human HepG22.2.15 cells after 3 days by neutral red dye-based plaque reduction assay, IC50=0.039μM | 26260336 | |
| MT4 | Antiviral assay | 5 days | Antiviral activity against HIV1 3B expressing wild type reverse transcriptase infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay, EC50=3.1μM | 27267005 | |
| HepG2.2.15.7 | Antiviral assay | 9 days | Antiviral activity against HBV infected in human HepG2.2.15.7 cells assessed as inhibition of viral DNA level after 9 days by real time PCR method, EC50=0.03μM | 27426303 | |
| MT4 | Antiviral assay | 5 days | Antiviral activity against wild type HIV1 3B harboring reverse transcriptase infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay, EC50=2.24μM | 27541578 | |
| MT4 | Antiviral assay | 5 days | Antiviral activity against HIV2 ROD harboring reverse transcriptase infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay, EC50=8.79μM | 27541578 | |
| HepG2(2.2.15) | Antiviral assay | 6 days | Antiviral activity against HBV ayw1 infected in human HepG2(2.2.15) cells assessed as reduction in viral replication by measuring intracellular viral DNA copy number after 6 days by real-time qPCR method, EC50<0.01μM | 27748590 | |
| HepG2(2.2.15) | Antiviral assay | 6 days | Antiviral activity against HBV ayw1 infected in human HepG2(2.2.15) cells assessed as reduction in viral replication by measuring extracellular viral DNA copy number after 6 days by real-time qPCR method, EC50=0.01μM | 27748590 | |
| MT4 | Antiviral assay | 5 days | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay, EC50=2.22μM | 27748590 | |
| MT4 | Antiviral assay | 5 days | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay, EC50=8.81μM | 27748590 | |
| HepAD38 | Antiviral assay | 5 days | Antiviral activity against HBV infected in human HepAD38 cells assessed as inhibition of DNA replication after 5 days by RT-PCR method, EC50=0.04μM | 28094179 | |
| P4R5 MAGI | Function assay | 2 hrs | Inhibition of HIV1 BaL dinucleoside reverse transcriptase infected in human P4R5 MAGI cells assessed as reduction in viral infection after 2 hrs by Galacto-Star beta-galactosidase reporter gene assay, EC50=11.3μM | 28351588 | |
| P4R5 MAGI | Function assay | 2 hrs | Inhibition of HIV1 3B dinucleoside reverse transcriptase infected in human P4R5 MAGI cells assessed as reduction in viral infection after 2 hrs by Galacto-Star beta-galactosidase reporter gene assay, EC50=32.7μM | 28351588 | |
| HepG2.2.15 | Antiviral assay | 8 days | Antiviral activity against Hepatitis B virus infected in human HepG2.2.15 cells assessed as inhibition of viral DNA replication after 8 days by real time fluorescent PCR method, IC50=0.5μM | 28494252 | |
| MT4 | Antiviral assay | 5 days | Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay, EC50=2.54μM | 28659246 | |
| HepG2(2.2.15) | Antiviral assay | 6 days | Antiviral activity against HBV ayw1 infected in human HepG2(2.2.15) cells assessed as reduction in viral replication by measuring intracellular viral DNA copy number after 6 days byr by real-time qPCR assay, EC50=0.00887μM | 28682067 | |
| HepG2(2.2.15) | Antiviral assay | 6 days | Antiviral activity against HBV ayw1 infected in human HepG2(2.2.15) cells assessed as reduction in viral replication by measuring extracellular viral DNA copy number after 6 days by real-time qPCR method, EC50=0.02μM | 28682067 | |
| SupT1 | Antiviral assay | 48 hrs | Antiviral activity against VSV-G pseudotyped HIV1 infected in human SupT1 cells after 48 hrs by luciferase reporter gene assay, IC50=0.1μM | 29016131 | |
| HepG2(2.2.15) | Antiviral assay | 6 days | Antiviral activity against HBV infected in human HepG2(2.2.15) cells assessed as inhibition of viral DNA replication after 6 days by RT-PCR method, IC50<0.1μM | 29288943 | |
| HepG2.2.15 | Antiviral assay | 6 days | Antiviral activity against Hepatitis B virus infected in human HepG2.2.15 cells assessed as reduction in extracellular viral DNA levels after 6 days by qPCR/TaqMan assay, IC50=0.025μM | 30286292 | |
| MT4 | Antiviral assay | 5 days | Antiviral activity against HIV1 RES056 containing reverse transcriptase K103N + Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay, EC50=7.77μM | 30606670 | |
| MT4 | Antiviral assay | 5 days | Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay, EC50=12.8μM | 30606670 | |
| MT4 | Antiviral assay | 5 days | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay, EC50=6.41μM | 30721060 | |
| C8166 | Antiviral assay | 72 hrs | Antiviral activity against HIV1 3B infected in human C8166 cells assessed as inhibition of syncytial cell formation incubated for 72 hrs, EC50=0.3μM | 31310115 | |
| MT4 | Antiviral assay | 5 days | Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay, EC50=1.92μM | 31434039 | |
| MT4 | Antiviral assay | 5 days | Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay, EC50=3.14μM | 31434039 | |
| MT4 | Antiviral assay | 5 days | Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay, EC50=3.58μM | 31434039 | |
| MT4 | Antiviral assay | 5 days | Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay, EC50=3.7μM | 31434039 | |
| MT4 | Antiviral assay | 5 days | Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay, EC50=3.88μM | 31434039 | |
| MT4 | Antiviral assay | 5 days | Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay, EC50=4.45μM | 31434039 | |
| MT4 | Antiviral assay | 5 days | Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay, EC50=4.54μM | 31434039 | |
| MT4 | Antiviral assay | 5 days | Antiviral activity against drug resistant HIV-1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay, EC50=5.54μM | 31434039 | |
| 2.2.15 | Function assay | In vitro effective concentration against hepatitis B virus was determined in 2.2.15 cells, EC50=0.008μM | 9301659 | ||
| PBMC | Anti-HIV-1 assay | Anti-HIV-1 activity against human peripheral blood mononuclear (PBM) cells infected with HIV-1 strain LAV, EC50=10.1μM | 8423591 | ||
| PBMC | Anti-HIV-1 assay | Anti-HIV-1 activity against human peripheral blood mononuclear (PBM) cells infected with HIV-1 strain LAV, EC50=0.21μM | 8423591 | ||
| PBMC | Anti-HIV-1 assay | Anti-HIV-1 activity against human peripheral blood mononuclear (PBM) cells infected with HIV-1 strain LAV, EC50=0.06μM | 8423591 | ||
| PBMC | Anti-HIV-1 assay | Anti-HIV-1 activity against human peripheral blood mononuclear (PBM) cells infected with HIV-1 strain LAV, EC50=0.0018μM | 8423591 | ||
| PBMC | Function assay | Concentration required for antiviral activity in PBMC (human peripheral blood mononuclear cells) infected with HIV-1 strain LAV, EC50=0.21μM | 8410975 | ||
| PBMC | Function assay | Concentration required for antiviral activity in PBMC (human peripheral blood mononuclear cells) infected with HIV-1 strain LAV, EC50=0.0018μM | 8410975 | ||
| MT-4 | Function assay | Concentration required to inhibit syntica formation by 50% in HIV-1 infected MT-4 cells, IC50=0.1μM | 8035429 | ||
| PBMC | Anti-HIV-1 assay | In vitro anti-HIV activity in peripheral blood mononuclear cells, EC50=0.07μM | 9301659 | ||
| 2.2.15 | Antiviral assay | Antiviral activity against Hepatitis B virus (HBV) in 2.2.15 cells, EC50=0.008μM | 11052795 | ||
| PBMC | Antiviral assay | Antiviral activity against Immunodeficiency virus type-1 (HIV-1) in peripheral blood mononuclear cells, EC50=0.07μM | 11052795 | ||
| H9 | Antiviral assay | Antiviral activity against HIV1 3B in human H9 cells assessed as inhibition of virus-induced cytopathic effect by formazan-based conventional colorimetric technique, EC50=0.06μM | 11430019 | ||
| H9 | Antiviral assay | Antiviral activity against HIV1 RF in human H9 cells assessed as inhibition of virus-induced cytopathic effect by formazan-based conventional colorimetric technique, EC50=0.06μM | 11430019 | ||
| PBMC | Antiviral assay | Antiviral activity against HIV-1xxBRU mutant strain in human PBM cells, EC90=0.08μM | 12383014 | ||
| PBMC | Function assay | Activity against Lamivudine-resistant virus (HIV-1XXBRU) in human PBM cells, expressed as EC50, EC50=0.035μM | 12852755 | ||
| PBMC | Function assay | In vitro concentration required to inhibit the HIV-1 LA1 replication on PBMCs cell (peripheral blood mononuclear cells), EC50=0.01μM | 12852943 | ||
| PBMC | Function assay | Effective concentration to inhibit HIV-1 LAI cytopathicity in PBMC cells was determined in vitro, EC50=0.0116μM | 14971898 | ||
| HepG2.2.15 | Function assay | Effective concentration to inhibit hepatitis B virus cytopathicity in HepG2.2.15 cells was determined in vitro, EC50=0.2μM | 14971898 | ||
| MT-4 | Function assay | Effective concentration to inhibit HIV-1 IIIB cytopathicity in MT-4 cells was determined in vitro, EC50=0.5μM | 14971898 | ||
| PBMC | Antiviral assay | Antiviral activity against wild type HIV virus(xxBRU) in Human peripheral blood mononuclear (PBM) cells, EC90=0.08μM | 15027854 | ||
| PBMC | Function assay | Effective concentration against Wild Type HIV-1 virus in human peripheral blood mononuclear cells, EC50=0.041μM | 15189036 | ||
| 2.2.15 | Function assay | Inhibition of HBV replication in 2.2.15 cells by DNA hybridization assay, EC50=0.02μM | 15615545 | ||
| 2.2.15 | Function assay | Effective concentration required to inhibit hepatitis B virus replication in 2.2.15 cells in DNA hybridization assay, EC50=0.05μM | 15634003 | ||
| PBMC | Function assay | In vitro effective concentration against Lamivudine resistant wild type HIV-1 in human peripheral blood mononuclear cells, EC50=0.027μM | 15916425 | ||
| PBMC | Function assay | In vitro effective concentration against Lamivudine resistant wild type HIV-1 in human peripheral blood mononuclear cells, EC90=0.25μM | 15916425 | ||
| 2.2.15 | Function assay | Effective concentrations at which 2-fold depression of extracellular virion DNA (HBV) was observed in 2.2.15 Cells, EC50=0.06μM | 16033283 | ||
| 2.2.15 | Function assay | Effective concentrations at which 2-fold depression of extracellular virion DNA (HBV) was observed in 2.2.15 Cells, EC90=0.17μM | 16033283 | ||
| 2.2.15 | Function assay | Effective concentrations at which 10-fold depression of intracellular intermediates of HBV DNA was observed in 2.2.15 Cells, EC50=0.23μM | 16033283 | ||
| 2.2.15 | Function assay | Effective concentrations at which 10-fold depression of intracellular intermediates of HBV DNA was observed in 2.2.15 Cells, EC90=0.69μM | 16033283 | ||
| 2.2.15 | Function assay | Inhibition of synthesis of extracellular virion DNA release in cultured human hepatoblastoma 2.2.15 cells, EC50=0.048μM | 16213713 | ||
| 2.2.15 | Function assay | Inhibition of synthesis of extracellular virion DNA release in cultured human hepatoblastoma 2.2.15 cells, EC90=0.151μM | 16213713 | ||
| 2.2.15 | Function assay | Inhibition of synthesis of intracellular HBV DNA replicative intermediates in cultured human hepatoblastoma 2.2.15 cells, EC50=0.251μM | 16213713 | ||
| 2.2.15 | Function assay | Inhibition of synthesis of intracellular HBV DNA replicative intermediates in cultured human hepatoblastoma 2.2.15 cells, EC90=0.648μM | 16213713 | ||
| 2.2.15 | Function assay | Inhibition of wild type HBV transfected in human hepatoblastoma 2.2.15 cells, EC50=2.1μM | 16539393 | ||
| hepatoma 2.2.15 | Antiviral assay | Antiviral activity against wild type HBV in human hepatoma 2.2.15 cells, EC50=2.1μM | 16759112 | ||
| 2.2.15 | Function assay | Inhibition of HBV replication in 2.2.15 cells by DNA hybridization assay, EC50=0.02μM | 17004726 | ||
| Huh7 | Function assay | Inhibition of wild type HBV replication in Huh7 cells, EC50=1μM | 17371827 | ||
| PBMC | Antiviral assay | Antiviral activity against HIV1 LAI in human PBM cells, EC50=0.026μM | 17403996 | ||
| PBMC | Antiviral assay | Antiviral activity against HIV1 LAI in human PBM cells, EC90=0.12μM | 17403996 | ||
| HepG2.2.15 | Antiviral assay | Antiviral activity against HBV in HepG2.2.15 cells assessed as decrease in extracellular viral DNA level by RT-PCR, EC50=0.1μM | 17404006 | ||
| HepG2(2.2.15) | Antiviral assay | Antiviral activity against HBV in ayw wild type HepG2(2.2.15) cells assessed as inhibition of viral DNA replication, IC50=0.05μM | 17488817 | ||
| HepG2(2.2.15) | Function assay | Inhibition of HBV promoter in human HepG2(2.2.15) cells by luciferase reporter gene assay, IC50=0.08μM | 17488817 | ||
| HepW10 | Antiviral assay | Antiviral activity against HBV in adriamycin-resistant wild type HepW10 cells assessed as inhibition of viral DNA replication, IC50=0.1μM | 17488817 | ||
| HBV-Met | Antiviral assay | Antiviral activity against HBV in mouse ayw wild type HBV-Met cells assessed as inhibition of viral DNA replication, IC50=0.2μM | 17488817 | ||
| MT2 | Antiviral assay | Antiviral activity against 0.005 MOI HIV1 NL4-3 harboring wild type RT infected in human MT2 cells, EC50=0.04μM | 18316521 | ||
| MT2 | Antiviral assay | Antiviral activity against HIV1 subtype B-3B infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA, EC50=0.047μM | 18316521 | ||
| PBMC | Antiviral assay | Antiviral activity against HIV1 subtype B-ASM 034 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA, EC50=0.071μM | 18316521 | ||
| PBMC | Antiviral assay | Antiviral activity against HIV1 subtype B-92US076 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA, EC50=0.081μM | 18316521 | ||
| MT2 | Antiviral assay | Antiviral activity against HIV1 infected in human MT2 cells assessed as inhibition of viral replication, IC50=0.6μM | 19596885 | ||
| HeLa P4/R5 | Antiviral assay | Antiviral activity against HIV1 infected in human HeLa P4/R5 cells assessed as inhibition of viral replication, IC50=0.78μM | 19596885 | ||
| TZM-bl | Antiviral assay | Antiviral activity against wild-type HIV1 pNL4-3 infected in TZM-bl cells by luciferase assay, EC50=0.65μM | 19704131 | ||
| HepG2.2.15 | Antiviral assay | Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as inhibition of viral DNA replication, IC50=0.22μM | 19897363 | ||
| MT2 | Antiviral assay | Antiviral activity against Human immunodeficiency virus 1 3B harboring reverse transcriptase M184V, M184I mutant infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected on day 14 after 4 passages by PCR analysis, EC50=0.8μM | 21115794 | ||
| MT2 | Antiviral assay | Antiviral activity against Human immunodeficiency virus 1 3B harboring reverse transcriptase M184V mutant infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected on day 14 after 4 passages by PCR analysis, EC50=0.8μM | 21115794 | ||
| MT2 | Antiviral assay | Antiviral activity against Human immunodeficiency virus 1 3B harboring reverse transcriptase M184V, M184I, K82N mutant infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected on day 14 after 4 passages by PCR analysi, EC50=0.8μM | 21115794 | ||
| HepG2(2.2.15) | Antiviral assay | Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as reduction in viral DNA by Southern blotting, EC50=0.06μM | 21333535 | ||
| HuH7 | Antiviral assay | Antiviral activity against wild type Hepatitis B virus infected in human HuH7 cells, EC50=0.056μM | 23237841 | ||
| HuH7 | Antiviral assay | Antiviral activity against wild type Hepatitis B virus infected in human HuH7 cells, EC90=0.142μM | 23237841 | ||
| HOG.R5 | Antiviral assay | Antiviral activity against HIV-1 3B/H9 infected in human HOG.R5 cells transfected with HIV1 LTR-GFP assessed as inhibition of viral replication by fluorescence analysis, IC50=1.2μM | 24404757 | ||
| MT4 | Antiviral assay | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post viral infection by MTT assay, EC50=2.442μM | 24794751 | ||
| MT4 | Antiviral assay | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post viral infection by MTT assay, EC50=7.2μM | 24794751 | ||
| HepG2.2.15 | Antiviral assay | Antiviral activity against hepatitis B virus infected in human HepG2.2.15 cells assessed as inhibition of viral replication, IC50=14.17μM | 25127104 | ||
| HepG2.2.15 | Antiviral assay | Antiviral activity against Hepatitis B virus infected in human HepG2.2.15 cells assessed as inhibition of HBV DNA replication by real-time fluorescence quantitative PCR analysis, IC50=6.86μM | 25847765 | ||
| Huh7 | Antiviral assay | Antiviral activity against lamivudine-resistant wild type hepatitis B virus infected in human Huh7 cells assessed as reduction in secreted DNA levels measured on day 7 by real-time PCR analysis, EC50=0.055μM | 28082068 | ||
| HepG2.215 | Antiviral assay | Antiviral activity against hepatitis B virus infected in human HepG2.215 cells assessed as reduction in viral DNA replication measured on day 7 by real time PCR analysis, EC50=0.1μM | 28082068 | ||
| Huh7 | Antiviral assay | Antiviral activity against lamivudine-resistant wild type hepatitis B virus infected in human Huh7 cells assessed as reduction in intracellular DNA levels measured on day 7 by real-time PCR analysis, EC50=0.237μM | 28082068 | ||
| HepG2.215 | Antiviral assay | Antiviral activity against hepatitis B virus infected in human HepG2.215 cells assessed as reduction in viral DNA replication measured on day 7 by real time PCR analysis, EC90=2μM | 28082068 | ||
| HepAD38 | Antiviral assay | Antiviral activity against HBV infected in human HepAD38 cells assessed as reduction in intracellular viral DNA level by RT-PCR method, EC50<0.01μM | 28688280 | ||
| HepAD38 | Antiviral assay | Antiviral activity against HBV infected in human HepAD38 cells assessed as reduction in viral replication by RT-PCR method, EC50=0.04μM | 28688280 | ||
| HepAD38 | Antiviral assay | Antiviral activity against HBV infected in human HepAD38 cells assessed as reduction in extracellular viral DNA level by RT-PCR method, EC50=0.04μM | 28688280 | ||
| HepAD38 | Antiviral assay | Antiviral activity against HBV infected in human HepAD38 cells assessed as reduction in viral replication by RT-PCR method, EC90=0.3μM | 28688280 | ||
| HepAD38 | Antiviral assay | Antiviral activity against HBV infected in human HepAD38 cells assessed as reduction in extracellular viral DNA level by RT-PCR method, EC90=0.3μM | 28688280 | ||
| HepAD38 | Antiviral assay | Antiviral activity against HBV infected in human HepAD38 cells assessed as reduction in intracellular viral DNA level by RT-PCR method, EC90=0.7μM | 28688280 | ||
| A549 | Antiviral assay | Antiviral activity against HIV1 virions derived from HIV/VSG-G or HIV/HA virions infected 293T cells using human A549 cells as target cells assessed as inhibition of viral replication using compound pre-mixed virions followed by incubation with target cel, IC50=0.51μM | 29699924 | ||
| HepG2.2.15 | Antiviral assay | Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as reduction in cytoplasmic DNA synthesis by reed and munch method, IC50=2.22μM | 31223460 | ||
| PBMC | Antiviral assay | Antiviral activity in PBM cells expressed as IC50, IC50=0.002μM | ChEMBL | ||
| HepG2.2.15 | Antiviral assay | Antiviral activity against hepatitis B virus in human hepatoma cell line (2.2.15 cells), EC50=0.01μM | ChEMBL | ||
| HepG2.2.15 | Function assay | Effective concentration necessary to decrease extracellular Hepatitis B virus DNA levels by 50% in human hepatoblastoma cell line (2.2.15 cells) in vitro, EC50=0.038μM | ChEMBL | ||
| PBMC | Function assay | Compound was tested for its anti-HIV activity against HIV-1 LAI in human peripheral blood mononuclear (PBM) cells, EC50=0.06μM | ChEMBL | ||
| HepG2.2.15 | Function assay | Effective concentration necessary to decrease extracellular Hepatitis B virus DNA levels by 90% in human hepatoblastoma cell line (2.2.15 cells) in vitro, EC90=0.16μM | ChEMBL | ||
| HepG2.2.15 | Function assay | Tested for the effective concentration required to inhibit HBV in HepG2.2.15 human liver cells, EC50=0.2μM | ChEMBL | ||
| PBMC | Antiviral assay | Antiviral activity in PBM cells, IC50=0.21μM | ChEMBL | ||
| PBMC | Antiviral assay | Antiviral activity in PBM cells expressed as IC50, IC50=0.21μM | ChEMBL | ||
| MT-4 | Antiviral assay | Antiviral activity in MT-4 cells, IC50=0.37μM | ChEMBL | ||
| MT-4 | Antiviral assay | Antiviral activity in MT-4 cells expressed as IC50, IC50=0.37μM | ChEMBL | ||
| MT-4 | Antiviral assay | Antiviral activity in MT-4 cells expressed as IC50, IC50=0.61μM | ChEMBL | ||
| MT-4 | Function assay | Compound was tested for its anti-HIV activity in acutely infected MT-4 cells, EC50=7μM | ChEMBL | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Lamivudine是一种有效的核苷类似物逆转录酶抑制剂，用于治疗慢性乙肝和艾滋病。它主要是通过阻滞HIV逆转录酶和乙肝病毒聚合酶发挥其作用。 | |
|---|---|---|
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | Lamivudine具有特异的抗脱氧胞苷激酶的活性，HBV聚合酶的非天然的L-构型的dNTP的不寻常的底物，而PCV的抗HBV活性似乎取决于几个因素，包括最佳磷酸（足够抗病毒活性，但不杀伤）由密钥细胞酶，PCV-TP的细胞内半衰期和PCV-TP的能力，抑制乙肝病毒的RT吸反应以及RT和DNA聚合酶活性。[1] Lamivudine和Penciclovir抑制鸭乙型肝炎病毒（DHBV）的复制，与单独使用时的效果类似，两个核苷类似物在很宽的范围内的临床相关浓度具有协同作用。Lamivudine和Penciclovir联用比单独两种药物更有效地减少DHBV的常顽固病毒共价闭合环状（CCC）DNA的形式。[2] 在PBMC 中，Lamivudine抑制HIV-I产生的p24抗原产量，ED50s从0.07 μM到0.2 μM。[3] |
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|---|---|---|---|---|
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06056596 | Recruiting | Retinal Detachment|Rhegmatogenous Retinal Detachment |
University of Wisconsin Madison |
January 2024 | Early Phase 1 |
| NCT04133012 | Completed | HIV-1 Infection |
ANRS Emerging Infectious Diseases|ViiV Healthcare |
February 10 2020 | Not Applicable |
| NCT03869944 | Active not recruiting | HIV-1 |
ANRS Emerging Infectious Diseases|Institut National de la Santé Et de la Recherche Médicale France|Centre Muraz |
December 4 2019 | Phase 2 |
化学信息&溶解度
| 分子量 | 229.26 | 分子式 | C8H11N3O3S |
| CAS号 | 134678-17-4 | SDF | Download Lamivudine SDF |
| Smiles | C1C(OC(S1)CO)N2C=CC(=NC2=O)N | ||
| 储存条件(自收到货起) | |||
|
体外溶解度 |
DMSO : 45 mg/mL ( (196.28 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : 45 mg/mL Ethanol : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
技术支持
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