| Identification | Back Directory | [Name]
GSK1265744 (sodiuM salt) | [CAS]
1051375-13-3 | [Synonyms]
Cabotegravir Sodium
Sodium Cabotegravir
GSK1265744 (sodiuM salt)
GSK1265744 (sodiuM salt) ISO 9001：2015 REACH
Sodium (3S,11aR)-8-((2,4-difluorobenzyl)carbamoyl)-3-methyl-5,7-dioxo-2,3,5,7,11,11a-hexahydrooxazolo[3,2-a]pyrido[1,2-d]pyrazin-6-olate
(3S,11AR)-N-(2,4-DIFLUOROBENZYL)-6-HYDROXY-3-METHYL-5,7-DIOXO-2,3,5,7,11,11A-HEXAHYDROOXAZOLO[3,2-A]PYRIDO[1,2-D]PYRAZINE-8-CARBOXAMIDE, SODIUM SALT | [Molecular Formula]
C19H18F2N3NaO5 | [MDL Number]
MFCD25976749 | [MOL File]
1051375-13-3.mol | [Molecular Weight]
429.36 |
| Chemical Properties | Back Directory | [storage temp. ]
4°C, away from moisture | [solubility ]
DMSO : 6.9 mg/mL (16.15 mM; ultrasonic and warming and heat to 60°C) | [form ]
Solid | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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 IC50 values of 2.5 nM, 0.41 μM and 0.81 μM for HIVADA, 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[1][2]. | [Definition]
ChEBI: Cabotegravir sodium is an organic sodium salt that is the monosodium salt of cabotegravir. Used for treatment of HIV-1. It has a role as a HIV-1 integrase inhibitor. It contains a cabotegravir(1-). | [in vivo]
The half-life of Cabotegravir is up to 54 days in mice[1].
Cabotegravir (25 or 50 mg/kg; i.v.; single dose or twice) protects Macaques against intravenous challenge with SIVmac251[4]. | [References]
[1] Zhou T, et al. Creation of a nanoformulated cabotegravir prodrug with improved antiretroviral profiles. Biomaterials. 2018 Jan;151:53-65. DOI:10.1016/j.biomaterials.2017.10.023
[2] Reese MJ, et al. Drug interaction profile of the HIV integrase inhibitor cabotegravir: assessment from in vitro studies and a clinical investigation with midazolam. Xenobiotica. 2016;46(5):445-56. DOI:10.3109/00498254.2015.1081993
[3] Yoshinaga T, et al. Antiviral characteristics of GSK1265744, an HIV integrase inhibitor dosed orally or by long-acting injection. Antimicrob Agents Chemother. 2015 Jan;59(1):397-406. DOI:10.1128/AAC.03909-14
[4] Andrews CD, et al. Cabotegravir long acting injection protects macaques against intravenous challenge with SIVmac251. AIDS. 2017 Feb 20;31(4):461-467. DOI:10.1097/QAD.0000000000001343 |
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