中文名称卡博特韦中文同义词卡博特韦自由酸;(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;卡博格韦;卡博特韦杂质;化合物GW1929;13C,2H2,15N]-卡博替拉韦;13C,2H5]-卡博替拉韦英文名称Cabotegravir(GSK744,GSK1265744)英文同义词GSK1265744;GSK744;(3S,11aR)-N-[(2,4-DifluorophChemicalbookenyl)methyl]-2,3,5,7,11,11a-hexahydro-6-hydroxy-3-methyl-5,7-dioxo-oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamide;Cabotegravir(GSK744,GSK1265744);CabotegravirFreeAcid;Cabotegravir;Cyclicpyranopterin;SK744,GSK1265744CAS号1051375-10-0分子式C19H17F2N3O5分子量405.35
博格韦卡博格韦是一种有效的HIV整合酶抑制剂，卡博格韦（Cabotegravir）可阻止HIV病毒感染人体细胞，而利匹韦林（Rilpivirine）则可阻止病毒复制自身。生物活性Cabotegravir(GSK744,GSK1265744)是一种长效HIVintegrase抑制剂，作用于广泛的HIV亚型，抑制了HIV-1integrase催化的链转移反应的IC50为3nM。Phase2。体外研究GSK1265744inhibitsHIVreplicationwithEC50of0.22nMand0.34-Chemicalbook1.3nMagainstHIV-1Ba-LandNL432,respectively.GSK1265744producescytotoxicitywithCC50of6.4,5.0,9.2,and13μMinproliferatingIM-9,U-937,MT-4,andMolt-4celllines,respectively.体内研究GSK1265744(50mg/kg)treatmentprotectsrhesusmacaquesagainstthreehigh-doseSHIVchallenges.
体外研究GSK1265744抑制HIV复制，对HIV-1Ba-L和NL432的EC50分别为0.22nM和0.34-1.3nM。GSK1265744在增殖的IM-9，U-937Chemicalbook，MT-4，和Molt-4细胞系中产生细胞毒性，CC50分别为6.4，5.0，9.2，和13μM。体内研究GSK1265744(50mg/kg)防止三个高剂量SHIV感染恒河猴。