Raltegravir
别名: MK-0518 中文名称：拉替拉韦，雷特格韦
Raltegravir是一种有效的integrase (IN)抑制剂，作用于WT和S217Q PFV IN，在无细胞试验中IC50分别为90 nM和40 nM。它对HIV-1 IN的选择性比对其他相关Mg2+依赖性酶要高1000倍以上，如HCV聚合酶、HIV反转录酶、HIV RNaseH、人类α-, β-, γ-聚合酶。
Raltegravir Chemical Structure
CAS: 518048-05-0
产品质控
批次：
纯度：
99.82%
99.82
Raltegravir相关产品
| 相关靶点 | HIV-1 Integrase HIV-2 Integrase HIV Integrase | 点击展开 |
|---|---|---|
| 相关产品 | MK-2048 BMS-707035 | 点击展开 |
| 相关化合物库 | 抗感染化合物库 抗生素化合物库 抗病毒化合物库 抗寄生虫药物库 肠道微生物代谢物库 | 点击展开 |
相关信号通路图
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 |
|---|---|---|---|---|---|
| U373-MAGI | Antiviral assay | 50 or 100 nM | 72 hrs | Antiviral activity against VSV-G pseudotyped HIV-1 NL4-3 infected in human U373-MAGI cells assessed as reduction in gag level at 50 or 100 nM measured at 72 hrs post infection by qPCR method | 27117260 |
| U373-MAGI | Antiviral assay | 50 or 100 nM | 72 hrs | Antiviral activity against VSV-G pseudotyped HIV-1 NL4-3 infected in human U373-MAGI cells assessed as reduction in U5-gag level at 50 or 100 nM measured at 72 hrs post infection by qPCR method | 27117260 |
| MT2 | Antiviral assay | 1 uM | 30 hrs | Antiviral activity against wild-type HIV1 NL4-3 infected infected in human MT2 cells assessed as reduction in HIV1 integrated DNA at 1 uM and measured after 30 hrs post infection by Alu-LTR PCR protocol based method | 30996780 |
| MT2 | Antiviral assay | 3 to 4 days | Antiviral activity against HIV1 NL4-3 infected in human MT2 cells measured after 3 to 4 days by luciferase reporter gene assay, EC50 = 0.002 μM. | 32081010 | |
| MT2 | Antiviral assay | 5 days | Antiviral activity against HIV1 3B infected in human MT2 cells after 5 days by chemiluminescence in presence of fetal bovine serum, EC50 = 0.004 μM. | 19285389 | |
| HOS | Antiviral assay | 3 hrs | Antiviral activity against wild-type Human immunodeficiency virus 1 infected in HOS cells preincubated for 3 hrs followed by viral infection measured after 48 hrs by luciferase reporter gene assay, EC50 = 0.004 μM. | 24471816 | |
| MT2 | Antiviral assay | 5 days | Antiviral activity against HIV1 3B in MT2 cells after 5 days, EC50 = 0.006 μM. | 18207398 | |
| MT4 | Function assay | 1 hr | Inhibition of wild type HIV1 3B infected in human MT4 cells using cells pre-incubated with compound for 1 hr measured 4 days post viral infection by MTT assay, IC50 = 0.0062 μM. | 22963135 | |
| MT4 | Antiviral assay | 48 to 72 hrs | Antiviral activity against HIV1 infected in human MT4 cells expressing GFP incubated for 48 to 72 hrs in absence of 50% normal human serum by multiple round viral replication kinetics assay, IP = 0.009 μM. | 26397965 | |
| HeLa | Antiviral assay | 48 hrs | Antiviral activity against VSV-G pseudotyped HIV1 lentiviral particles infected in human HeLa cells incubated for 48 hrs by spectrofluorometry, IC50 = 0.01 μM. | 22858300 | |
| cat FL-4 | Antiviral assay | 7 days | Antiviral activity against Feline immunodeficiency virus infected in cat FL-4 cells assessed as inhibition of viral replication after 7 days by quantitative RT-PCR analysis, EC50 = 0.01 μM. | 25702849 | |
| cat FL-4 | Antiviral assay | 7 days | Antiviral activity against FIV infected in cat FL-4 cells assessed as reduction in viral RNA level measured after 7 days by qRT-PCR analysis, EC50 = 0.01 μM. | 31395510 | |
| BL21(DE3) | Function assay | 1 hr | Inhibition of recombinant HIV-1 integrase stand transfer activity expressed in Escherichia coli BL21(DE3) cells using 32P-labeled DNA substrate after 1 hr by densitometric analysis, IC50 = 0.013 μM. | 26451771 | |
| MT4 | Antiviral assay | 5 days | Antiviral activity against HIV1 3B infected in human MT4 cells incubated for 5 days by MTT assay, EC50 = 0.015 μM. | 31324562 | |
| MT-4 | Antiviral assay | 5 days | Antiviral activity against HIV1 3B/LAI infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect measured survival after 5 days by MTT assay, EC50 = 0.016 μM. | 24124919 | |
| HeLa-CD4-LTR-beta-gal | Antiviral assay | 1 day | Antiviral activity against HIV-1 3B infected in human HeLa-CD4-LTR-beta-gal cells after 1 day by spectroscopic analysis, EC50 = 0.016 μM. | 25629256 | |
| MT2 | Antiviral assay | 5 days | Antiviral activity against HIV1 3B infected in human MT2 cells after 5 days by chemiluminescence in presence of human serum albumin, EC50 = 0.02 μM. | 19285389 | |
| MT4 | Antiviral assay | 5 days | Antiviral activity against HIV2 ROD infected in human MT4 cells incubated for 5 days by MTT assay, EC50 = 0.02 μM. | 31324562 | |
| TZM-b1 | Antiviral assay | 1 hr | Antiviral activity against HIV-1 NL4.3 infected in human TZM-b1 cells pretreated for 1 hr followed by viral infection measured after 2 days by CPRG assay, IC50 = 0.021 μM. | 28408224 | |
| CEM-SS | Antiviral assay | 6 days | Antiviral activity against HIV1 3B infected in human CEM-SS cells assessed as reduction of virus-induced cytopathic effect after 6 days by MTS assay, EC50 = 0.023 μM. | 27283261 | |
| HeLa | Antiviral assay | 3 days | Antiviral activity against HIV1 3B infected in human HeLa cells expressing CD4-LTR-beta-gal assessed as inhibition of viral replication after 3 days by reporter gene assay, EC50 = 0.0236 μM. | 24684270 | |
| HeLa | Antiviral assay | 2 days | Antiviral activity against HIV1 3B infected in human HeLa cells expressing CD4 assessed as inhibition of viral replication after 2 days by beta-galactosidase reporter gene assay, EC50 = 0.024 μM. | 24124919 | |
| TZM-bl | Antiviral assay | 48 hrs | Antiviral activity against Human immunodeficiency virus 1 infected in human TZM-bl cells assessed as inhibition of viral replication after 48 hrs by inverted microscopic analysis, EC50 = 0.025 μM. | 22154762 | |
| MT4 | Function assay | 1 hr | Inhibition of wild type HIV1 3B infected in human MT4 cells using cells pre-incubated with compound for 1 hr measured 4 days post viral infection in presence of 20 mg/ml HSA by MTT assay, IC50 = 0.029 μM. | 22963135 | |
| P4R5 MAGI | Antiviral assay | 24 hrs | Antiviral activity against HIV1 infected in CD4/CXCR4/CCR5 expressing human P4R5 MAGI cells preincubated with cells for 24 hrs followed by viral infection measured after 48 hrs by beta-galactosidase reporter gene assay, EC50 = 0.03 μM. | 30031976 | |
| P4R5 | Antiviral assay | 24 hrs | Antiviral activity against HIV1 infected in CD4/CXCR4/CCR5 expressing human P4R5 cells assessed as inhibition of viral replication preincubated with cells for 24 hrs followed by viral infection measured after 48 hrs by beta-galactosidase reporter gene ass, EC50 = 0.03 μM. | 28525279 | |
| P4R5 | Antiviral assay | 24 hrs | Antiviral activity against HIV1 infected in human P4R5 cells assessed as reduction in viral infection preincubated with cells for 24 hrs followed by viral infection measured after 48 hrs by fluorescence based beta-galactosidase reporter gene based MAGI as, EC50 = 0.03 μM. | 29031062 | |
| P4R5 | Antiviral assay | 24 hrs | Antiviral activity against HIV-1 infected in human P4R5 cells assessed as reduction in viral replication preincubated for 24 hrs followed by viral infection and measured after 48 hrs by MAGI assay, EC50 = 0.03 μM. | 30739822 | |
| P4R5 | Antiviral assay | 24 hrs | Antiviral activity against HIV1 infected in human P4R5 cells assessed as reduction of virus replication preincubated with cells for 24 hrs followed by viral infection for 48 hrs by 4-methylumbelliferylgalactoside-based MAGI assay, EC50 = 0.03 μM. | 27283261 | |
| MT4 | Antiviral assay | 48 to 72 hrs | Antiviral activity against HIV1 infected in human MT4 cells expressing GFP incubated for 48 to 72 hrs in presence of 50% normal human serum by multiple round viral replication kinetics assay, IP = 0.053 μM. | 26397965 | |
| BL21(DE3) | Function assay | 1 hr | Inhibition of LEDGF/p75-dependent full length HIV-1 integrase expressed in Escherichia coli BL21(DE3) cells preincubated for 1 hr further incubated for 90 mins with biotin-labeled donor DNA and target DNA by HTRF assay, IC50 = 0.058 μM. | 31442684 | |
| HeLa-T4 | Antiviral assay | 48 hrs | Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef infected in human HeLa-T4 cells assessed as luciferase activity after 48 hrs by exogenous RT assay, EC50 = 0.077 μM. | 21060108 | |
| TZM-bl | Antiviral assay | 48 hrs | Antiviral activity against HIV-1 infected in human TZM-bl cells assessed as inhibition of viral replication for 48 hrs by bright-Glo luciferase assay, EC50 = 0.15 μM. | 26487913 | |
| HOS | Antiviral assay | 3 hrs | Antiviral activity against Human immunodeficiency virus 1 harboring integrase N155H mutant infected in HOS cells preincubated for 3 hrs followed by viral infection measured after 48 hrs by luciferase reporter gene assay, EC50 = 0.154 μM. | 24471816 | |
| HOS | Antiviral assay | 3 hrs | Antiviral activity against Human immunodeficiency virus 1 harboring integrase Y143R mutant infected in HOS cells preincubated for 3 hrs followed by viral infection measured after 48 hrs by luciferase reporter gene assay, EC50 = 0.162 μM. | 24471816 | |
| TZM-bl | Antiviral assay | 1 hr | Antiviral activity against HIV1 NL4.3 infected in human TZM-bl cells expressing CXCR4-tropic incubated for 1 hr prior to infection measured after 48 hrs by luciferase reporter gene assay, IC50 = 0.5 μM. | 24291042 | |
| TZM-bl | Antiviral assay | 1 hr | Antiviral activity against HIV1 NL4.3 infected in human TZM-bl cells expressing CXCR4-tropic incubated for 1 hr prior to infection measured after 48 hrs by luciferase reporter gene assay, IC50 = 0.50119 μM. | 24291042 | |
| HeLa-T4 | Antiviral assay | 48 hrs | Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef infected in human HeLa-T4 cells assessed as luciferase activity after 48 hrs by exogenous RT assay, EC95 = 0.81 μM. | 21060108 | |
| HOS | Antiviral assay | 3 hrs | Antiviral activity against Human immunodeficiency virus 1 harboring integrase G140S/Q148H double mutant infected in HOS cells preincubated for 3 hrs followed by viral infection measured after 48 hrs by luciferase reporter gene assay, EC50 = 1.9 μM. | 24471816 | |
| MT2 | Antiviral assay | 3 to 4 days | Antiviral activity against HIV1 NL4-3 harboring G140S/Q148H mutant infected in human MT2 cells measured after 3 to 4 days by luciferase reporter gene assay, EC50 = 2.42 μM. | 32081010 | |
| HeLaT4 | Antiviral assay | 24 hrs | Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef assessed as level of infection using human HeLaT4 cells pretreated for 24 hrs followed by exposed to vi, EC50 = 4.6 μM. | 21060108 | |
| MT4 | Cytotoxicity assay | 5 days | Cytotoxicity in mock-infected human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay, CC50 = 6.51 μM. | 31324562 | |
| MT-4 | Antiviral assay | Antiviral activity against vesicular stomatitis virus G-pseudotyped Human immunodeficiency virus infected in human MT-4 cells assessed as inhibition of viral replication, EC50 = 0.002 μM. | 18160521 | ||
| MT-4 | Antiviral assay | Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT-4 cells assessed as inhibition of viral replication, EC50 = 0.0018 μM. | 18160521 | ||
| MT4 | Antiviral assay | Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as inhibition of viral replication, EC50 = 0.0014 μM. | 18541726 | ||
| MT-2 | Antiviral assay | Antiviral activity against HIV1 3B infected in human MT-2 cells by two fold dilution method in presence of 10% FBS, EC50 = 0.003 μM. | 19104010 | ||
| HOS | Antiviral assay | Antiviral activity against HIV1 harboring wild-type integrase infected in human HOS cells, EC50 = 0.004 μM. | 21493066 | ||
| MT-4 | Antiviral assay | Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50 = 0.006 μM. | 18378713 | ||
| MT4 | Antiviral assay | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50 = 0.006 μM. | 24900718 | ||
| MT4 | Antiviral assay | Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay, EC50 = 0.006 μM. | 24793360 | ||
| MT4 | Antiviral assay | Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect, EC50 = 0.0061 μM. | 20479206 | ||
| MT4 | Antiviral assay | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction of virus-induced cytopathogenicity by MTT assay, EC50 = 0.0064 μM. | 19447621 | ||
| MT-4 | Antiviral assay | Antiviral activity against HIV 1 NL4.3 harboring integrase L74M mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50 = 0.007 μM. | 18378713 | ||
| MT4 | Antiviral assay | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of viral-induced cytopathic effect by MTT assay, EC50 = 0.0078 μM. | 28951095 | ||
| MT-4 | Antiviral assay | Antiviral activity against HIV1 3B infected in human MT-4 cells by two fold dilution method in presence of 10% FBS, EC50 = 0.008 μM. | 19104010 | ||
| MT-4 | Antiviral assay | Antiviral activity against HIV 1 NL4.3 integrase S230N mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50 = 0.009 μM. | 18378713 | ||
| FL-4 | Antiviral assay | Antiviral activity against Feline immunodeficiency virus infected in cat FL-4 cells assessed as viral RNA production by RT-qPCR, EC50 = 0.00998 μM. | 24813732 | ||
| MT-4 | Antiviral assay | Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 20 passages selected in presence of compound, EC50 = 0.01 μM. | 18378713 | ||
| MT4 | Antiviral assay | Antiviral activity against HIV2 ROD 3B infected in human MT4 cells assessed as inhibition of viral-induced cytopathic effect by MTT assay, EC50 = 0.011 μM. | 28951095 | ||
| MT4 | Antiviral assay | Antiviral activity against Human immunodeficiency virus 1 3B infected in MT4 cells assessed as protection against virus-induced cytopathic effect measured 5 days post infection by MTT assay, EC50 = 0.0117 μM. | 29940462 | ||
| MT4 | Antiviral assay | Antiviral activity against HIV1 3B assessed as inhibition of viral-induced cytopathic effect in human MT4 cells, EC50 = 0.013 μM. | 18417342 | ||
| MT4 | Antiviral assay | Antiviral activity against HIV1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect, EC50 = 0.013 μM. | 20630765 | ||
| MT4 | Antiviral assay | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50 = 0.013 μM. | 21227550 | ||
| MT-4 | Antiviral assay | Antiviral activity against HIV 1 NL4.3 integrase E92Q mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50 = 0.015 μM. | 18378713 | ||
| MT2 | Antiviral assay | Antiviral activity against HIV in MT2 cells in presence of 35 mg/mL human serum albumin, EC50 = 0.016 μM. | 18207398 | ||
| MT-2 | Antiviral assay | Antiviral activity against HIV1 3B infected in human MT-2 cells by two fold dilution method in presence of 10% FBS, HSA and alpha1-AGP, EC50 = 0.018 μM. | 19104010 | ||
| MT4 | Antiviral assay | Antiviral activity against HIV1 3B in human MT4 cells in presence of 10% heat-activated fetal bovine serum, IC95 = 0.019 μM. | 18763751 | ||
| HeLa-CD4-LTR-beta-gal | Antiviral assay | Antiviral activity against HIV-1 3B infected in human HeLa-CD4-LTR-beta-gal cells assessed as inhibition of viral replication by SpectraMax GEMINI-XS plate reader analysis, EC50 = 0.0236 μM. | 25961960 | ||
| MT-4 | Antiviral assay | Antiviral activity against HIV 1 RIN HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 40 passages selected in presence of compound, EC50 = 0.025 μM. | 18378713 | ||
| MT4 | Antiviral assay | Antiviral activity against HIV1 3B in human MT4 cells in presence of 50% normal human serum, IC95 = 0.031 μM. | 18763751 | ||
| MT-4 | Antiviral assay | Antiviral activity against HIV 1 RIN HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 60 passages selected in presence of compound, EC50 = 0.068 μM. | 18378713 | ||
| HeLaT4 | Antiviral assay | Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef assessed as level of 2 mins magnetic nanopartials-medated infection in human HeLaT4 cells treated for 1, EC91 = 0.073 μM. | 21060108 | ||
| TZM-bl | Antiviral assay | Antiviral activity against HIV1 NL4.3 infected in human TZM-bl cells measured upto 24 hrs by bright Glo-luciferase reporter gene assay, IC50 = 0.16 μM. | 31557609 | ||
| CHO | Function assay | Inhibition of slow delayed inward rectifying potassium current (Iks) in Chinese Hamster Ovary (CHO) cells expressing hKvLQT1/hminK measured using IonWorks Quattro automated patch clamp platform, IC50 = 25.1189 μM. | 25087753 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Raltegravir是一种有效的integrase (IN)抑制剂，作用于WT和S217Q PFV IN，在无细胞试验中IC50分别为90 nM和40 nM。它对HIV-1 IN的选择性比对其他相关Mg2+依赖性酶要高1000倍以上，如HCV聚合酶、HIV反转录酶、HIV RNaseH、人类α-, β-, γ-聚合酶。 | ||||
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| 特性 | Raltegravir 是第一个被批准的人类免疫缺陷病毒1型（HIV-1）整合酶抑制剂。 | ||||
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | PFV整合携带S217H替换的IN，之后对 Raltegravir 的敏感性降低10倍，IC50为900 nM。PFV IN 具有10% WT 活性，且被Raltegravir抑制，IC50为200 nM,说明与 WT IN相比，对整合酶（IN）链转移抑制剂(INSTI)的敏感性降低约2倍。S217Q PFV IN 对 Raltegravir的敏感性至少与WT 酶相似。[1] Raltegravir由葡萄糖醛酸化，而不是肝脏代谢而来。Raltegravir 在体外作用于人类T 淋巴细胞培养物，有效作用于HIV-1，抑制达95%时浓度为31±20 nM。Raltegravir作用于 CEMx174细胞，也有效作用于HIV-2,IC95为6 nM。Raltegravir 代谢主要通过葡萄糖醛酸化。葡萄糖醛酸化酶的强诱导剂UGT1A1显著降低 Raltegravir 浓度。Raltegravir 微弱抑制肝细胞色素 P450。Raltegravir不会诱导 CYP3A4 RNA 表达或 CYP3A4依赖的睾丸激素 6-β-羟化酶活性。[2]在镁和钙存在时，Raltegravir细胞扩散性降低。[3]Raltegravir 和相关的HIV-1整合酶 (IN) 链转移抑制剂 (INSTIs) 高效阻断病毒复制。[4] Raltegravir 作用于急性感染人类淋巴 CD4+ T细胞系MT-4和 CEMx174, 高效抑制SIVmac251复制，EC90处于低纳摩尔范围。[5] | |||
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| 激酶实验 | PFV 整合实验 | |||
| 为了定量分析链转移，供体DNA底物通过退火 HPLC 级寡核苷酸 5′-GACTCACTATAGGGCACGCGTCAAAATTCCATGACA 和 5′-ATTGTCATG GAATTTTGACGCGTGCCCTATAGTGAGTC而形成。反应(40 μL) 含0.75 μM PFV IN, 0.75 μM 供体 DNA, 4 nM (300 ng) 超螺旋 pGEM9-Zf(−) 靶 DNA, 125 mM NaCl, 5 mM MgSO4, 4 μM ZnCl2, 10 mM DTT, 0.8% (vol/vol) DMSO, 和 25 mM BisTris 丙烷–HCl, pH 7.45。加入指定浓度Raltegravir。加入2 μL PFV IN （在150 mM NaCl, 2 mM DTT, 和 10 mM Tris-HCl, pH 7.4中稀释）开始反应,在 37oC下反应1小时后，加入25 mM EDTA 和 0.5% (wt/vol) SDS终止反应。反应产物通过与 20 μg 蛋白酶 K 在 37oC下消化30分钟而脱蛋白，随后使用乙醇 沉淀,在 在1.5％琼脂糖凝胶上分离，然后通过用溴化乙锭染色观察。通过实时定量PCR, 使用 Platinum SYBR Green qPCR SuperMix 和三种引物 : 5′-CTACTTACTCTAGCTTCCCGGCAAC, 5′-TTCGCCAGTTAATAGTTTGCGCAAC, 和 5′-GACTCACTATAGGGCACGCGT定量分析整合产物。PCR 反应 (20 μL) 含0.5 μM 每种引物和1 μL 稀释的整合反应产物。在95oC下进行5分钟变性，在CFX96 PCR仪上进行35次循环，再在95oC下变性10秒，在56oC下退火30秒，在68oC下延伸1分钟。在INSTI存在时，使用连续稀释的WT PFV IN 反应，获得标准曲线。 | ||||
| 细胞实验 | 细胞系 | 人类MT-4 细胞 | ||
| 浓度 | 0.0001 μM -1 μM | |||
| 孵育时间 | 2小时 | |||
| 方法 | 使用 SIVmac251, HIV-1 (IIIB) 和 HIV-2 (CDC 77618)对人类MT-4细胞进行多重感染2小时。然后在PBS中冲洗细胞3次，在有或无一系列一式三份Raltegravir 浓度 (0.0001 μM -1 μM)时，按5 × 105/mL 悬浮在含新鲜培养基 (在原代细胞中加入 50 单位/mL IL-2 ) 的96孔板中。也制备未治疗的感染对照和模拟感染对照，用于比较不同处理法得到的实验数据。通过MTT法(MT-4/MTT实验 )定量分析致MT-4细胞死亡的病毒。显微镜检测发现病毒感染的细胞培养物由于缺乏成簇的能力而大量死亡。移液打断成簇，在 37oC下温育2小时后, 通过光学显微镜l (100 × 放大倍数)观察新簇形成。通过ELISA收集细胞培养上清液，用于测量HIV-1 p24 和 HIV-2/SIVmac251 p27核心抗原。在CEMx174感染的细胞培养物中，具有病毒包膜糖蛋白诱导形成多核体的倾向,按盲实验形式计数多核体，感染5天后，通过光学显微镜观察每孔。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | CHOP / ATF-4 / XBP-1 / Lamin B |
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24625618 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | Raltegravir 作用于携带 SIVmac251感染的非人类灵长类动物，提高病毒-免疫。Raltegravir单独给药非人类灵长类动物后，检测不到病毒载量。[5] | |
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| 动物实验 | Animal Models | 印度猕猴 |
| Dosages | 50 mg/kg 或 100 mg/kg, 每天两次 | |
| Administration | 口服处理 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT04513626 | Recruiting | HIV Infections |
Centre de Recherches et d''Etude sur la Pathologie Tropicale et le Sida |
September 15 2020 | Phase 2 |
| NCT03667547 | Completed | Human Immunodeficiency Virus (HIV) Infection |
Merck Sharp & Dohme LLC |
September 27 2018 | Phase 4 |
| NCT03174977 | Recruiting | HIV-1-infection |
University of California San Francisco|Merck Sharp & Dohme LLC |
April 1 2018 | Early Phase 1 |
化学信息&溶解度
| 分子量 | 444.42 | 分子式 | C20H21FN6O5 |
| CAS号 | 518048-05-0 | SDF | Download Raltegravir SDF |
| Smiles | CC1=NN=C(O1)C(=O)NC(C)(C)C2=NC(=C(C(=O)N2C)O)C(=O)NCC3=CC=C(C=C3)F | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 89 mg/mL ( (200.26 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
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体内溶解配方 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。
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