Cabotegravir (GSK744, GSK1265744)

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产品名称:Cabotegravir (GSK744, GSK1265744)

CAS:1051375-10-0

别名：(3S,11AR)-N-[(2,4-二氟苯基)甲基]-2,3,5,7,11,11A-六氢-6-羟基-3-甲基-5,7-二氧代恶唑并[3,2-A]吡啶并[1,2-D]吡嗪-8-甲酰胺;卡博特韦自由酸;卡博特韦

英文名：Cabotegravir (GSK744, GSK1265744)

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生物活性Cabotegravir (GSK744, GSK1265744)是一种长效HIV integrase抑制剂，作用于广泛的HIV亚型，抑制了HIV-1 integrase 催化的链转移反应的IC50为3 nM。Phase 2。
体外研究GSK1265744 inhibits HIV replication with EC50 of 0.22 nM and 0.34-1.3 nM against HIV-1 Ba-L and NL432, respectively. GSK1265744 produces cytotoxicity with CC50 of 6.4, 5.0, 9.2, and 13 μM in proliferating IM-9, U-937, MT-4, and Molt-4 cell lines, respectively.
体内研究GSK1265744 (50 mg/kg) treatment protects rhesus macaques against three high-dose SHIV challenges.