Dolutegravir,GSK1349572  1051375-16-6德羅特韋(GSK-1349572,DTG)

德羅特韋(GSK-1349572,DTG)
分子式：C20H19F2N3O5    分子量：419.38
 
產(chǎn)品描述
S/GSK1349572 (GSK1349572) 是HIV integrase抑制劑，IC50為2.7 nM, 適度有效作用于抗Raltegravir的顯著突變體Y143R, Q148K, N155H, 和 G140S/Q148H。
靶點(diǎn)
HIV integrase
         
IC50
2.7 nM
         
體外研究
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.
體內(nèi)研究
 
溶解性
DMSO 84 mg/mL，水 <1 mg/mL，乙醇 <1 mg/mL
穩(wěn)定性
2年 -20°C粉狀，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.