中文名 | Cabotegravir |
英文名 | Cabotegravir |
别名 | 卡博特韦 卡博格韦 卡博特韦杂质 卡博特韦自由酸 化合物GW1929 (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 |
英文别名 | GSK744 GSK1265744 Cabotegravir SK744, GSK1265744 Cyclic pyranopterin Cabotegravir Free Acid Cabotegravir (GSK744, GSK1265744) (3S,11aR)-N-[(2,4-Difluorophenyl)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 |
CAS | 1051375-10-0 |
化学式 | C19H17F2N3O5 |
分子量 | 405.35 |
密度 | 1.57±0.1 g/cm3(Predicted) |
沸点 | 664.0±55.0 °C(Predicted) |
溶解度 | DMSO: 12.67 mg/mL |
酸度系数 | 4.50±1.00(Predicted) |
存储条件 | -20℃ |
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. GSK1265744抑制HIV复制,对HIV-1 Ba-L 和 NL432的EC50分别为0.22 nM和0.34-1.3 nM。GSK1265744在增殖的IM-9,U-937,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13 μM。 |
体内研究 | GSK1265744 (50 mg/kg) treatment protects rhesus macaques against three high-dose SHIV challenges. GSK1265744 (50 mg/kg)防止三个高剂量SHIV感染恒河猴。 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.467 ml | 12.335 ml | 24.67 ml |
5 mM | 0.493 ml | 2.467 ml | 4.934 ml |
10 mM | 0.247 ml | 1.233 ml | 2.467 ml |
5 mM | 0.049 ml | 0.247 ml | 0.493 ml |
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