HIV integrase IC502.7 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.
