德罗特韦(GSK-1349572,DTG)

产品描述

S/GSK1349572 (GSK1349572)是HIVintegrase抑制剂，IC50为2.7 nM,适度有效作用于抗Raltegravir的显著突变体Y143R, Q148K, N155H,和G140S/Q148H。

靶点

HIV integrase

IC50

2.7 nM

体外研究

S/GSK1349572 shows the potent inhibitory effect on nine clinical isolates from integrase inhibitor-na?ve HIV-2-infected patients with EC50 ranging from 0.2 nM -1.4 nM.[1]In vitro, S/GSK1349572 inhibits recombinant HIV-1 integrase-catalyzed strand transfer with IC50 of 2.7 nM. Furthermore, S/GSK1349572 potently inhibits HIV replication in cells such as peripheral blood mononuclear cells (PBMCs), MT-4 cells and CIP4 cells infected with a self-inactivating PHIV lentiviral vector with EC50 of 0,51 nM, 0.71 nM and 2.2 nM, respectively.In vitro, S/GSK1349572 exhibits potent activity against five different nonnucleoside reverse transcription inhibitor–resistant or nucleoside reverse transcription inhibitor–resistant viruses with EC50 ranging from 1.3 nM -2.1 nM. Similarly to that against wild-type virus, S/GSK1349572 shows equivalent activity against two protease inhibitor-resistant viruses with EC50 of 0.36 nM and 0.37 nM, respectively.

体内研究

溶解性

DMSO 84 mg/mL，水<1 mg/mL，乙醇<1 mg/mL

稳定性

2年-20°C粉状，6月-80°C溶于DMSO

特征

S/GSK1349572 (GSK1349572) is a next-generation and two-metal-binding HIV integrase strand transfer inhibitor.