Integrase
信号通路图
研究领域
抑制剂选择性比较
Integrase产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S2005 |
Raltegravir (MK-0518)Raltegravir (MK-0518)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。 |
a: HCV, hepatitis C virus; HBV, hepatitis B virus. B: PI, protease inhibitor; NRTI, nucleoside reverse transcriptase inhibitor; NNRTI, nonnucleoside reverse transcriptase inhibitor; IN, integrase inhibitor. c: n=3. d: The EC50 for samatasvir in the presence of 45% human serum was 25 pM.
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| S2001 |
Elvitegravir (GS-9137, JTK-303)Elvitegravir (GS-9137, JTK-303)是一种HIV抑制剂，作用于HIV-1 IIIB，HIV-2 EHO和HIV-2 ROD，无细胞试验中IC50 分别为0.7，2.8和1.4 nM。 |
PhA efflux in MDCKII-BCRP cells. Concentration-dependent inhibition of BCRP/ABCG2 by elvitegravir and vicriviroc. Each curve depicts one representative experiment of a series of three or four; each concentration was tested in 30000 cells.
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| S2667 |
Dolutegravir (GSK1349572)Dolutegravir (GSK1349572)是一种两个金属结合的HIVintegrase抑制剂，无细胞试验中IC50为2.7 nM，对耐Raltegravir的显著突变体Y143R，Q148K，N155H，和G140S/Q148H具有适度的活性。 |
qPCR kinetics of 2-LTRc and integrated DNA forms during a single round of HIV replication in the presence of inhibitors. MT4cells were infected with HIV-1 in the absence (DMSO) or in the presence of 100 nM EFV, 500 nM RAL, 500 nM DTG, 10 μM RDS1611, 10 μM RDS1644, 10 μM RDS1823 added at the time of infection (black bar) or 16 h p.i. (grey bar). Samples were analyzed for (A) total viral DNA at 24 h and (B) 2-LTRc and (C) integrated viral DNA at 48 h. The graph represents the average and standard deviation of three independent experiments. Significant at: p value < 0.05 (*); p value < 0.01 (**); p value < 0.001 (***); p value < 0.0001 (****).
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| S1366 |
BMS-707035BMS-707035是一种特异性的HIV-I integrase (IN)（整合酶）抑制剂，IC50为15 nM。Phase 2。 |
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| S2765 |
MK-2048MK-2048是一种有效的integrase(IN)和INR263K抑制剂，IC50分别为2.6 nM和1.5 nM。 |
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| S5911New |
BictegravirBictegravir是一种新型的、有效的HIV-1 integrase抑制剂。 |
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| S5245New |
Raltegravir potassiumRaltegravir Potassium是一种具有口服活性的raltegravir钾盐。Raltegravir是HIV-1 integrase抑制剂。 |
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| S7766 |
Cabotegravir (GSK744, GSK1265744)Cabotegravir (GSK744, GSK1265744)是一种长效HIV integrase抑制剂，作用于广泛的HIV亚型，抑制了HIV-1 integrase 催化的链转移反应的IC50为3 nM。Phase 2。 |
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| S4642 |
Dolutegravir SodiumDolutegravir是HIV整合酶抑制剂，IC50为2.7 nM。 |
Comparison of the activity of dolutegravir (DTG), raltegravir (RAL), and elvitegravir (EVG) against wild-type HIV-2ROD9. Values for RAL and EVG include data from two previously-published studies of HIV-2 from our group [14,15] plus additional determinations; all data were obtained using the single-cycle assay. Bars indicate mean 50% effective concentrations (EC50); the number of independent determinations (n) for each strain is shown below the x-axis. P values were obtained via analysis of variance (ANOVA) of log10-transformed EC50 values with Tukey’s post test (Prism v6.0). No cytotoxic effects were observed in dolutegravir-treated MAGIC-5A cultures at concentrations as high as 10,000 nM.
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| S4187 |
SalicylanilideSalicylanilides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。 |
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S2005 |
Raltegravir (MK-0518)Raltegravir (MK-0518)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。 |
a: HCV, hepatitis C virus; HBV, hepatitis B virus. B: PI, protease inhibitor; NRTI, nucleoside reverse transcriptase inhibitor; NNRTI, nonnucleoside reverse transcriptase inhibitor; IN, integrase inhibitor. c: n=3. d: The EC50 for samatasvir in the presence of 45% human serum was 25 pM.
|
|
| S2001 |
Elvitegravir (GS-9137, JTK-303)Elvitegravir (GS-9137, JTK-303)是一种HIV抑制剂，作用于HIV-1 IIIB，HIV-2 EHO和HIV-2 ROD，无细胞试验中IC50 分别为0.7，2.8和1.4 nM。 |
PhA efflux in MDCKII-BCRP cells. Concentration-dependent inhibition of BCRP/ABCG2 by elvitegravir and vicriviroc. Each curve depicts one representative experiment of a series of three or four; each concentration was tested in 30000 cells.
|
|
| S2667 |
Dolutegravir (GSK1349572)Dolutegravir (GSK1349572)是一种两个金属结合的HIVintegrase抑制剂，无细胞试验中IC50为2.7 nM，对耐Raltegravir的显著突变体Y143R，Q148K，N155H，和G140S/Q148H具有适度的活性。 |
qPCR kinetics of 2-LTRc and integrated DNA forms during a single round of HIV replication in the presence of inhibitors. MT4cells were infected with HIV-1 in the absence (DMSO) or in the presence of 100 nM EFV, 500 nM RAL, 500 nM DTG, 10 μM RDS1611, 10 μM RDS1644, 10 μM RDS1823 added at the time of infection (black bar) or 16 h p.i. (grey bar). Samples were analyzed for (A) total viral DNA at 24 h and (B) 2-LTRc and (C) integrated viral DNA at 48 h. The graph represents the average and standard deviation of three independent experiments. Significant at: p value < 0.05 (*); p value < 0.01 (**); p value < 0.001 (***); p value < 0.0001 (****).
|
|
| S1366 |
BMS-707035BMS-707035是一种特异性的HIV-I integrase (IN)（整合酶）抑制剂，IC50为15 nM。Phase 2。 |
||
| S2765 |
MK-2048MK-2048是一种有效的integrase(IN)和INR263K抑制剂，IC50分别为2.6 nM和1.5 nM。 |
||
| S5911New |
BictegravirBictegravir是一种新型的、有效的HIV-1 integrase抑制剂。 |
||
| S5245New |
Raltegravir potassiumRaltegravir Potassium是一种具有口服活性的raltegravir钾盐。Raltegravir是HIV-1 integrase抑制剂。 |
||
| S7766 |
Cabotegravir (GSK744, GSK1265744)Cabotegravir (GSK744, GSK1265744)是一种长效HIV integrase抑制剂，作用于广泛的HIV亚型，抑制了HIV-1 integrase 催化的链转移反应的IC50为3 nM。Phase 2。 |
||
| S4642 |
Dolutegravir SodiumDolutegravir是HIV整合酶抑制剂，IC50为2.7 nM。 |
Comparison of the activity of dolutegravir (DTG), raltegravir (RAL), and elvitegravir (EVG) against wild-type HIV-2ROD9. Values for RAL and EVG include data from two previously-published studies of HIV-2 from our group [14,15] plus additional determinations; all data were obtained using the single-cycle assay. Bars indicate mean 50% effective concentrations (EC50); the number of independent determinations (n) for each strain is shown below the x-axis. P values were obtained via analysis of variance (ANOVA) of log10-transformed EC50 values with Tukey’s post test (Prism v6.0). No cytotoxic effects were observed in dolutegravir-treated MAGIC-5A cultures at concentrations as high as 10,000 nM.
|
|
| S4187 |
SalicylanilideSalicylanilides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。 |
