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Dolutegravir sodium

CAS No. : 1051375-19-9

MCE 國(guó)際站：Dolutegravir sodium

產(chǎn)品活性：Dolutegravir sodium (S/GSK1349572 sodium) 是一種高效、口服的 HIV 整合酶鏈轉(zhuǎn)移抑制劑，在 HIV-1 整合酶催化的鏈轉(zhuǎn)移中的 IC₅₀ 值為 2.7 nM，Dolutegravir sodium (S/GSK1349572 sodium) 抑制 HIV-1 病毒在外周血單個(gè)核細(xì)胞中的復(fù)制，IC₅₀ 為 0.51 nM。Dolutegravir sodium (S/GSK1349572 sodium) 對(duì) Y143R，N155H 和 G140S/Q148H 突變體也保持高效 (EC₅₀=3.6-5.8 nM)。

研究領(lǐng)域：Metabolic Enzyme/Protease  |  Anti-infection

作用靶點(diǎn)：HIV Integrase  |  HIV

In Vitro: The EC₅₀ of Dolutegravir (S/GSK1349572) against HIV-1 is 0.51 nM in PBMCs, 0.71 nM in MT-4 cells, and 2.2 nM in the PHIV assay, which uses a pseudotyped self-inactivating virus. The 50% cytotoxic concentrations (CC₅₀) for Dolutegravir in proliferating IM-9, U-937, MT-4, and Molt-4 cells are 4.8, 7.0, 14, and 15 μM, respectively. In unstimulated and stimulated PBMCs, the CC₅₀ are 189 μM and 52 μM, respectively. Based on the EC₅₀ of Dolutegravir against HIV-1 in PBMCs (i.e., 0.51 nM), this translates to a cell-based therapeutic index of at least 9,400.

In Vivo: 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 (V_SS) 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 (C_max 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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