Dolutegravir (GSK1349572),1051375-16-6

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产品名称：Dolutegravir (GSK1349572)

产品别名：度鲁特韦

英文别名：S/GSK1349572;GSK1349572

靶点：HIV integrase

CAS：1051375-16-6

纯度：>98%

外观：白色至浅黄色固体

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

S/GSK1349572 (GSK 1349572) is a novel potent integrase inhibitor with an IC50 of 2.7 nM in vitro. S/GSK1349572 (GSK 1349572) is a compound for the treatment of HIV infection. S/GSK1349572 (GSK 1349572) exhibited in vitro activity against most clinical isolates obtained from patients failing RAL-based therapy. In PBMC cell assay, S/GSK1349572 inhibited HIV integrase with the antiviral IC50=0.51 and IC90=2.0 nM. In MT-4 antiviral assays, potency shift extrapolated to human serum was 75-fold providing PA-IC90=152 nM in PBMCs. S/GSK1349572 (GSK 1349572) had a markedly different resistance profile as evidenced by limited cross-resistance to RAL-resistant molecular clones, by its in vitro activity against clinical isolates obtained from patients failing RAL-based therapy, and in selecting different mutations with low level FC during serial passage. In vitro experiments support the potential for S/GSK1349572 (GSK 1349572) to have a higher genetic barrier to resistance when compared to 1st generation integrase inhibitors.

溶解性：DMSO ：77 mg/mL (183.6 mM)

体外研究：

S/GSK1349572 shows the potent inhibitory effect on nine clinical isolates from integrase inhibitor-naive HIV-2-infected patients with EC50 ranging from 0.2 nM -1.4 nM. 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：Following a single intravenous (IV) administration of Dolutegravir, the plasma clearance is low in rats (0.23 mL/min/kg) and monkeys (2.12 mL/min/kg). The half-lives in the rat and monkey are similar, approximately 6 h, and the steady-state volume of distribution (VSS) is low. Following oral administration, Dolutegravir is rapidly absorbed with a high oral bioavailability when administered as a solution to fasted male rats and a single monkey (75.6 and 87.0%, respectively). Dolutegravir exposure (Cmax and AUC) increased with increasing dose following oral administration of a suspension to non-fasted rats up to 250 mg/kg and non-fasted monkeys up to 50 mg/kg, although the increase is less than proportional.

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