Reverse Transcriptase

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研究领域

抑制剂选择性比较

Reverse Transcriptase产品

所有产品 Reverse Transcriptase抑制剂(28) 新Reverse Transcriptase产品

产品目录	产品描述	文献引用	实验数据
S1401	Tenofovir Tenofovir 对reverse transcriptase（逆转录酶）和B型肝炎病毒感染具有抑制作用。	Cell Death Dis, 2019, 10(6):419 Nat Med, 2018, 24(5):604-609 J Pharm Sci, 2017, 106(3):906-919	The Nucleotide analog reverse-transcriptase inhibitor Tenofovir disoproxil fumarate was added to TZM-bl cells. Cells were inoculated with 0.05 ng mock-exposed and semen-exposed HIV, and 0.5 ng HIV as infectivity-matched control. Infection rates were measured 3 days post infection by measuring β-galactosidase or or 4 days post infection by measuring luciferase activities. The left panels show the mean enzyme activities ± standard deviation derived from triplicate infections. RLU/s: relative light units per second. Middle panels show normalized infection rates in which reporter enzyme activities obtained from infected cells in the absence of inhibitor were set at 100%. The right panels depict the calculated IC50 values. The number above the bar represents the fold-change in the IC50 derived from 0.05 ng semen-exposed relative to 0.05 or 0.5 ng mock-exposed virus infection. Ns, no statistically significant difference; ** p<0.0001; * p<0.001 (unpaired t-test).
S1400	Tenofovir Disoproxil Fumarate Tenofovir Disoproxil Fumarate 属于一类抗逆转录病毒药物，其通过与天然底物脱氧腺苷5’-三磷酸盐竞争以及整合到DNA后终止DNA链抑制HIV reverse transcriptase活性。	Nanoscale, 2017, 9(44):17263-17273 Eur J Pharmacol, 2017, 811:155-163 Retrovirology, 2015, 10.1186/s12977-015-0139-7	Human PBMCs containing indicated concentrations of Tenofovir disoproxil fumarate were inoculated with 5 ng mock-exposed or semen-exposed R5-HIV-luciferase, or 50 ng R5-HIV-luciferase as infectivity matched control. Infection rates were determined 3 days post inoculation.
S1704	Emtricitabine Emtricitabine (FTC)是一种新型的核苷剂，对人类免疫缺陷病毒HIV和HBV具有抑制活性。是逆转录酶抑制剂，在细胞中的半衰期为39 h。	Nat Med, 2018, 24(5):604-609 J Clin Invest, 2017, 127(12):4352-4364 J Immunol, 2014, 193(7):3577-89
S1252	Entecavir Hydrate Entecavir，一个新的脱氧鸟嘌呤核苷类似物，是乙肝病毒复制的选择性抑制剂。	Oncotarget, 2017, 8(15):24694-24705 J Hepatol, 2015, 10.1016/j.jhep.2015.02.048
S1718	Adefovir Dipivoxil Adefovir Dipivoxil 抑制逆转录酶（丙型肝炎病毒（HBV）在体内复制的关键酶）。	Oncotarget, 2017, 8(15):24694-24705
S6492^New	Doravirine (MK-1439) Doravirine (MK-1439)是HIV-1单核苷酸逆转录酶抑制剂，对野生型逆转录酶和携带有K103N、Y181C突变的逆转录酶的IC50分别为12 nM、9.7 nM和9.7 nM。它十分特异，很少有脱靶效应。
S6452^New	Delavirdine (mesylate) Delavirdine Mesylate是delavirdine的甲磺酸盐形式。Delavirdine是一种合成的、非核苷类逆转录酶抑制剂。
S1742	Nevirapine Nevirapine 是一种非核苷逆转录酶抑制剂(NNRTI)，用于治疗HIV-1感染和AIDS。	PLoS One, 2018, 13(3):e0194611 Sci Transl Med, 2014, 6(262):262ra157	Cells were inoculated with 0.05 ng mock-exposed and semen-exposed HIV, and 0.5 ng HIV as infectivity-matched control. Infection rates were measured 3 d post infection by measuring β-galactosidase. Left: the mean enzyme activities. Middle: normalized infection rates in which reporter enzyme activities obtained from infected cells in the absence of nevirapine were set at 100%. Right: IC50 values.
S1702	Didanosine Didanosine是一种逆转录酶抑制剂，IC50为0.49 μM。	PLoS One, 2018, 13(3):e0194611 Cancer Cell, 2017, 32(2):221-237
S1706	Lamivudine 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。	Oncotarget, 2017, 8(15):24694-24705	The indicated liver cancer cell lines—Hep-3B, Huh-7 and PLC were treated with or without 5 types anti-hepatitis B virus drugs (C) with the concentration of 100 μM, and M1 virus (MOI = 10) for 72 hours. Following 72 hours, cell viabilities were determined by MTT assay (mean ± SD). N.S. Not significant.
S1398	Stavudine (d4T) Stavudine (d4T)是一种核苷类似物逆转录酶抑制剂（NARTI），有效作用于HIV。
S1651	Telbivudine Telbivudine是一种HBV逆转录酶抑制剂，用于治疗乙型肝炎感染。	Oncotarget, 2017, 8(15):24694-24705 Sci Rep, 2013, 3:2105
S3080	Etravirine (TMC125) Etravirine (TMC125)是一种非核苷类逆转录酶抑制剂(NNRTI)，用于治疗HIV。	Antiviral Res, 2017, 145:103-113 Antiviral Res, 2016, 126:90-8 Biochemistry, 2016, 55(28):3864-73	1D 19F NMR spectra of RT181tfmF and several RT181tfmF mutants in the absence (black) and presence of NVP (pink), EFV (green), ETR (blue) and RPV (orange). (A) Superposition of the 19F spectra of apo-RT181tfmF and the 19F spectra of RT181tfmF in the presence of each NNRTI, (B) Superposition of the 19F spectra of apo-RT181tfmF-V108I and the 19F spectra of RT181tfmF in the presence of each NNRTI, (C) Superposition of the 19F spectra of apo-RT181tfmF-K103N and the 19F spectra of RT181tfmF-K103N in the presence of each NNRTI, (D) Superposition of the 19F spectra of apo-RT181tfmF-E138K(p51) and the 19F spectra of RT181tfmF-E138K(p51) in the presence of each NNRTI. The 19F spectra in the presence of each NNRTI at 1:1 and 1:5 molar ratios are shown in light and dark colors, respectively. Chemical formulae for each inhibitor are depicted in the individual panels.
S2579	Zidovudine Zidovudine是一种逆转录酶抑制剂。它能够降低同源重组效率。Zidovudine降低了CRISPR介导的特定序列基因组敲入效率，但增强了其敲除效率。	PLoS One, 2018, 13(3):e0194611 Cancer Cell, 2017, 32(2):221-237
S1719	Zalcitabine Zalcitabine是一种核苷类HIV逆转录酶抑制剂(NARTI)。
S3165	Abacavir sulfate Abacavir sulfate是一种常用的核苷类似物，具有抗HIV-1病毒活性。Abacavir是一种鸟嘌呤类似物，它的靶点是病毒的反转录酶。
S2914	Dapivirine (TMC120) Dapivirine (TMC120)是一种非核苷类抑制剂，作用于HIV逆转录酶，IC50为24 nM，抑制多种不同类型的HIV-1分离株，包括多种耐NNRTI的分离株。Phase 3。	Mol Pharm, 2017, 14(8):2660-2669 Antimicrob Agents Chemother, 2017, 61(7)
S3076	Foscarnet Sodium Foscarnet Sodium通过非竞争性抑制dNTPs而抑制病毒RNA聚合酶，逆转录酶，DNA聚合酶。	Neuron, 2017, 96(6):1290-1302
S7303	Rilpivirine Rilpivirine是非核苷逆转录抑制剂(NNRTI)，被用于治疗HIV-1感染。	Biomed Chromatogr, 2018, 10.1002/bmc.4274 Antiviral Res, 2017, 145:103-113 Antimicrob Agents Chemother, 2017, 61(7)
S4890	Bifendate Bifendate, a synthetic intermediate of schisandrin C, is an anti-HBV drug used in Chinese medicine for the treatment of chronic hepatitis B.
S5215	Abacavir Abacavir (ABC) is a powerful nucleoside analog reverse transcriptase inhibitor (NRTI) used to treat HIV and AIDS.	Antiviral Res, 2017, 142:123-135 Antiviral Res, 2015, 123:62-9 Antimicrob Agents Chemother, 2014, 58(8):4804-13
S5246	Entecavir Entecavir, a new deoxyguanine nucleoside analogue, is a selective inhibitor of the replication of the hepatitis B virus (HBV).
S4187	Salicylanilide Salicylanilides是一组具有广泛的生物活性的化合物，具有抗病毒效力，抗菌（包括抗分枝杆菌），和抗真菌活性。
S4685	Efavirenz Efavirenz是一种合成的、非核苷类逆转录酶抑制剂，具有抗病毒活性。
S3606	Fangchinoline Fangchinoline是双苄基异喹啉类生物碱，是HIV-1的新型抑制剂，具有缓解疼痛、降低血压和抗菌活性。
S7856	Tenofovir Alafenamide (GS-7340) Tenofovir Alafenamide (GS-7340)是tenofovir的前药，tenofovir是一种reverse transcriptase抑制剂，用于治疗HIV和乙型肝炎。
S5423	4-Chloro-2-(trifluoroacetyl)aniline hydrochloride 4-Chloro-2-(trifluoroacetyl)aniline hydrochloride is a HIV-1 RT (HIV reverse transcriptase) inhibitor.
S5068	Adefovir Adefovir is an orally administered nucleotide analog reverse transcriptase inhibitor used for treatment of hepatitis B and herpes simplex virus infection.

产品目录	产品描述	文献引用	实验数据
S1401	Tenofovir Tenofovir 对reverse transcriptase（逆转录酶）和B型肝炎病毒感染具有抑制作用。	Cell Death Dis,2019, 10(6):419 Nat Med,2018, 24(5):604-609 J Pharm Sci,2017, 106(3):906-919	The Nucleotide analog reverse-transcriptase inhibitor Tenofovir disoproxil fumarate was added to TZM-bl cells. Cells were inoculated with 0.05 ng mock-exposed and semen-exposed HIV, and 0.5 ng HIV as infectivity-matched control. Infection rates were measured 3 days post infection by measuring β-galactosidase or or 4 days post infection by measuring luciferase activities. The left panels show the mean enzyme activities ± standard deviation derived from triplicate infections. RLU/s: relative light units per second. Middle panels show normalized infection rates in which reporter enzyme activities obtained from infected cells in the absence of inhibitor were set at 100%. The right panels depict the calculated IC50 values. The number above the bar represents the fold-change in the IC50 derived from 0.05 ng semen-exposed relative to 0.05 or 0.5 ng mock-exposed virus infection. Ns, no statistically significant difference; ** p<0.0001; * p<0.001 (unpaired t-test).
S1400	Tenofovir Disoproxil Fumarate Tenofovir Disoproxil Fumarate 属于一类抗逆转录病毒药物，其通过与天然底物脱氧腺苷5’-三磷酸盐竞争以及整合到DNA后终止DNA链抑制HIV reverse transcriptase活性。	Nanoscale,2017, 9(44):17263-17273 Eur J Pharmacol,2017, 811:155-163 Retrovirology,2015, 10.1186/s12977-015-0139-7	Human PBMCs containing indicated concentrations of Tenofovir disoproxil fumarate were inoculated with 5 ng mock-exposed or semen-exposed R5-HIV-luciferase, or 50 ng R5-HIV-luciferase as infectivity matched control. Infection rates were determined 3 days post inoculation.
S1704	Emtricitabine Emtricitabine (FTC)是一种新型的核苷剂，对人类免疫缺陷病毒HIV和HBV具有抑制活性。是逆转录酶抑制剂，在细胞中的半衰期为39 h。	Nat Med,2018, 24(5):604-609 J Clin Invest,2017, 127(12):4352-4364 J Immunol,2014, 193(7):3577-89
S1252	Entecavir Hydrate Entecavir，一个新的脱氧鸟嘌呤核苷类似物，是乙肝病毒复制的选择性抑制剂。	Oncotarget,2017, 8(15):24694-24705 J Hepatol,2015, 10.1016/j.jhep.2015.02.048
S1718	Adefovir Dipivoxil Adefovir Dipivoxil 抑制逆转录酶（丙型肝炎病毒（HBV）在体内复制的关键酶）。	Oncotarget,2017, 8(15):24694-24705
S6492^New	Doravirine (MK-1439) Doravirine (MK-1439)是HIV-1单核苷酸逆转录酶抑制剂，对野生型逆转录酶和携带有K103N、Y181C突变的逆转录酶的IC50分别为12 nM、9.7 nM和9.7 nM。它十分特异，很少有脱靶效应。
S6452^New	Delavirdine (mesylate) Delavirdine Mesylate是delavirdine的甲磺酸盐形式。Delavirdine是一种合成的、非核苷类逆转录酶抑制剂。
S1742	Nevirapine Nevirapine 是一种非核苷逆转录酶抑制剂(NNRTI)，用于治疗HIV-1感染和AIDS。	PLoS One,2018, 13(3):e0194611 Sci Transl Med,2014, 6(262):262ra157	Cells were inoculated with 0.05 ng mock-exposed and semen-exposed HIV, and 0.5 ng HIV as infectivity-matched control. Infection rates were measured 3 d post infection by measuring β-galactosidase. Left: the mean enzyme activities. Middle: normalized infection rates in which reporter enzyme activities obtained from infected cells in the absence of nevirapine were set at 100%. Right: IC50 values.
S1702	Didanosine Didanosine是一种逆转录酶抑制剂，IC50为0.49 μM。	PLoS One,2018, 13(3):e0194611 Cancer Cell,2017, 32(2):221-237
S1706	Lamivudine 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。	Oncotarget,2017, 8(15):24694-24705	The indicated liver cancer cell lines—Hep-3B, Huh-7 and PLC were treated with or without 5 types anti-hepatitis B virus drugs (C) with the concentration of 100 μM, and M1 virus (MOI = 10) for 72 hours. Following 72 hours, cell viabilities were determined by MTT assay (mean ± SD). N.S. Not significant.
S1398	Stavudine (d4T) Stavudine (d4T)是一种核苷类似物逆转录酶抑制剂（NARTI），有效作用于HIV。
S1651	Telbivudine Telbivudine是一种HBV逆转录酶抑制剂，用于治疗乙型肝炎感染。	Oncotarget,2017, 8(15):24694-24705 Sci Rep,2013, 3:2105
S3080	Etravirine (TMC125) Etravirine (TMC125)是一种非核苷类逆转录酶抑制剂(NNRTI)，用于治疗HIV。	Antiviral Res,2017, 145:103-113 Antiviral Res,2016, 126:90-8 Biochemistry,2016, 55(28):3864-73	1D 19F NMR spectra of RT181tfmF and several RT181tfmF mutants in the absence (black) and presence of NVP (pink), EFV (green), ETR (blue) and RPV (orange). (A) Superposition of the 19F spectra of apo-RT181tfmF and the 19F spectra of RT181tfmF in the presence of each NNRTI, (B) Superposition of the 19F spectra of apo-RT181tfmF-V108I and the 19F spectra of RT181tfmF in the presence of each NNRTI, (C) Superposition of the 19F spectra of apo-RT181tfmF-K103N and the 19F spectra of RT181tfmF-K103N in the presence of each NNRTI, (D) Superposition of the 19F spectra of apo-RT181tfmF-E138K(p51) and the 19F spectra of RT181tfmF-E138K(p51) in the presence of each NNRTI. The 19F spectra in the presence of each NNRTI at 1:1 and 1:5 molar ratios are shown in light and dark colors, respectively. Chemical formulae for each inhibitor are depicted in the individual panels.
S2579	Zidovudine Zidovudine是一种逆转录酶抑制剂。它能够降低同源重组效率。Zidovudine降低了CRISPR介导的特定序列基因组敲入效率，但增强了其敲除效率。	PLoS One,2018, 13(3):e0194611 Cancer Cell,2017, 32(2):221-237
S1719	Zalcitabine Zalcitabine是一种核苷类HIV逆转录酶抑制剂(NARTI)。
S3165	Abacavir sulfate Abacavir sulfate是一种常用的核苷类似物，具有抗HIV-1病毒活性。Abacavir是一种鸟嘌呤类似物，它的靶点是病毒的反转录酶。
S2914	Dapivirine (TMC120) Dapivirine (TMC120)是一种非核苷类抑制剂，作用于HIV逆转录酶，IC50为24 nM，抑制多种不同类型的HIV-1分离株，包括多种耐NNRTI的分离株。Phase 3。	Mol Pharm,2017, 14(8):2660-2669 Antimicrob Agents Chemother,2017, 61(7)
S3076	Foscarnet Sodium Foscarnet Sodium通过非竞争性抑制dNTPs而抑制病毒RNA聚合酶，逆转录酶，DNA聚合酶。	Neuron,2017, 96(6):1290-1302
S7303	Rilpivirine Rilpivirine是非核苷逆转录抑制剂(NNRTI)，被用于治疗HIV-1感染。	Biomed Chromatogr,2018, 10.1002/bmc.4274 Antiviral Res,2017, 145:103-113 Antimicrob Agents Chemother,2017, 61(7)
S4890	Bifendate Bifendate, a synthetic intermediate of schisandrin C, is an anti-HBV drug used in Chinese medicine for the treatment of chronic hepatitis B.
S5215	Abacavir Abacavir (ABC) is a powerful nucleoside analog reverse transcriptase inhibitor (NRTI) used to treat HIV and AIDS.	Antiviral Res,2017, 142:123-135 Antiviral Res,2015, 123:62-9 Antimicrob Agents Chemother,2014, 58(8):4804-13
S5246	Entecavir Entecavir, a new deoxyguanine nucleoside analogue, is a selective inhibitor of the replication of the hepatitis B virus (HBV).
S4187	Salicylanilide Salicylanilides是一组具有广泛的生物活性的化合物，具有抗病毒效力，抗菌（包括抗分枝杆菌），和抗真菌活性。
S4685	Efavirenz Efavirenz是一种合成的、非核苷类逆转录酶抑制剂，具有抗病毒活性。
S3606	Fangchinoline Fangchinoline是双苄基异喹啉类生物碱，是HIV-1的新型抑制剂，具有缓解疼痛、降低血压和抗菌活性。
S7856	Tenofovir Alafenamide (GS-7340) Tenofovir Alafenamide (GS-7340)是tenofovir的前药，tenofovir是一种reverse transcriptase抑制剂，用于治疗HIV和乙型肝炎。
S5423	4-Chloro-2-(trifluoroacetyl)aniline hydrochloride 4-Chloro-2-(trifluoroacetyl)aniline hydrochloride is a HIV-1 RT (HIV reverse transcriptase) inhibitor.
S5068	Adefovir Adefovir is an orally administered nucleotide analog reverse transcriptase inhibitor used for treatment of hepatitis B and herpes simplex virus infection.

研究领域

产品类型

Reverse Transcriptase

信号通路图

研究领域

抑制剂选择性比较

Reverse Transcriptase产品