Cabotegravir (GSK-1265744) sodium is a orally active and long-acting HIV integrase strand transfer inhibitor and organic anion transporter 1/3 ( OAT1 / OAT3 ) inhibitor with IC 50 values of 2.5 nM, 0.41 μM and 0.81 μM for HIV ADA , OAT3 and OAT1, respectively. Cabotegravir sodium is primarily metabolized by uridine diphosphate glucuronosyltransferase (UGT) 1A1, with low potential to interact with other antiretroviral agents (ARVs). Cabotegravir sodium can be used to research AIDS In Vitro Cabotegravir (GSK-1265744) inhibits the HIV-1 integrase catalyzed strand transfer reaction with an IC 50 of 3.0 nM in vitro. The antiviral EC 50 against HIV-1 Ba-L is 0.22 nM and that against NL432 is 0.34 nM in PBMCs, 0.57 nM using CellTiter-Glo and 1.3 nM using MTT in MT-4, and 0.5 nM in the PHIV assay, which uses a pseudotyped self-inactivating virus. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: MT-4 cells Concentration: 0-32 nM Incubation Time: 4 or 5 days Result: Showed antiviral activity with an EC 50 of 1.3 nM. In Vivo The half-life of Cabotegravir is up to 54 days in mice . Cabotegravir (25 or 50 mg/kg; i.v.; single dose or twice) protects Macaques against intravenous challenge with SIVmac251. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:IC 50 : 2.5 nM (HIV ADA ), IC 50 : 0.41 μM (OAT3), 0.81 μM (OAT1)
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Cabotegravir sodium
CAS number：1051375-13-3 molecular formula：C19H16F2N3NaO5
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| Chinese alias | 卡博特韦钠 | ||
| English alias | Q27257476 | Cabotegravir (sodium) | CABOTEGRAVIR SODIUM [ORANGE BOOK] | EN300-97513 | F11513 | Tox21_111391 | Cabotegravir sodium | Oxazolo(3,2-a)pyrido(1,2-d)pyrazine-8-carboxamide, N-((2,4-difluorophenyl)methyl)-2,3,5,7,11,11a-hexahydro-6-hydroxy-3-meth | ||
| CAS number | 1051375-13-3 | molecular formula | C19H16F2N3NaO5 |
| molecular weight | 427.33 g/mol | Exact mass | ≥99% |
| PSA | 102.000 Ų | logp | - |
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