| 应用 |
A potent integrase strand transfer inhibitor for (PFV) IN. |
| 产品介绍 |
Raltegravir (MK-0518)是一种有效的整合酶链转移抑制剂，作用于WT和S217Q原型泡沫病毒(PFV)整合酶，IC50分别为90 nM和40 nM。 |
| 备注 |
Raltegravir (MK-0518, Isentress) is a potent integrase (IN) inhibitor for WT and S217Q PFV IN with IC50 of 90 nM and 40 nM, respectively. |
| 生化机理 |
Raltegravir is a potent HIV-1 integrase inhibitor. Raltegravir sensitizes S217Q PFV IN to the same extent as the WT enzyme. Raltegravir is potently active against HIV-1 in vitro. Raltegravir is also active against HIV-2 in CEMx174 cells. Raltegravir weakly inhibits hepatic cytochrome P450 activity. Raltegravir effectively attenuates viral replication. Raltegravir efficiently inhibits SIVmac251 replication in acutely infected human lymphoid CD4+ T-cell lines MT-4 and CEMx174. |
| 别名 |
雷特格韦; N-(2-(4-(4-氟苄基氨基甲酰基)-5-羟基-1-甲基-6-氧代-1,6-二氢嘧啶-2-基)丙-2-基)-5-甲基-1,3,4-恶二唑-2-甲酰胺;Isentress;N-(2-(4-(4-Fluorobenzylcarbamoyl)-5-hydroxy-1-methyl-6-oxo-1,6-dihydropyrimidin-2-yl)propan-2-yl)-5-methyl-1,3,4-oxadiazole-2-carboxamide; N-((4-Fluorophenyl)methyl)-1,6-dihydro-5-hydroxy-1-methyl-2-(1-methyl-1-(((5-methyl-1,3,4-oxadiazol-2-yl)carbonyl)amino)ethyl)-6-oxo-4-pyrimidinecarboxamide |
2850412321
