货号:A115208
同义名:
GSK-1265744; S/GSK1265744
Cabotegravir is a potent HIV integrase inhibitor as an oral lead-in tablet and long-acting injectable for the treatment and prevention of HIV infection. Cabotegravir is an inhibitor of OAT1 (IC50 0.81 μM) and OAT3 (IC50 0.41 μM).
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描述 | Cabotegravir (GSK-1265744) operates as an orally available, long-acting inhibitor of the HIV integrase strand transfer and the organic anion transporters 1 and 3 (OAT1/OAT3), with IC50s of 2.5 nM for HIVADA, 0.41 μM for OAT3, and 0.81 μM for OAT1. Its metabolism is mainly via the uridine diphosphate glucuronosyltransferase (UGT) 1A1, presenting minimal interaction risks with other antiretroviral drugs (ARVs), making it suitable for AIDS researc[1].[2]. |
Animal study | Cabotegravir administered intravenously at doses of either 25 or 50 mg/kg, once or twice, effectively shields Macaques from an intravenous SIVmac251 challenge[4]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.47mL 0.49mL 0.25mL |
12.34mL 2.47mL 1.23mL |
24.67mL 4.93mL 2.47mL |
CAS号 | 1051375-10-0 |
分子式 | C19H17F2N3O5 |
分子量 | 405.35 |
SMILES Code | O=C(C1=CN(C2=C(O)C1=O)C[C@](OC[C@@H]3C)([H])N3C2=O)NCC4=CC=C(F)C=C4F |
MDL No. | MFCD25976748 |
别名 | GSK-1265744; S/GSK1265744; GSK1265744A; GSK744 |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry,2-8°C |