Cabotegravir sodium

CAS: 1051375-13-3 F: C19H16F2N3NaO5 W: 427.33

Cabotegravir (GSK-1265744) sodium is a orally active and long-acting HIV integrase strand transfer inhibitor and organic

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Bioactivity	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 drugs (ARVs). Cabotegravir sodium can be used to research AIDS[1][2].
Target	IC50: 2.5 nM (HIVADA)IC50: 0.41 μM (OAT3), 0.81 μM (OAT1)
Invitro	Cabotegravir (GSK-1265744) 在体外抑制 HIV-1 整合酶催化的链转移反应，IC50 为 3.0 nM。在 PBMCs中对 HIV-1 Ba-L 的抗病毒 EC50为 0.22 nM，对 NL432 的EC50 为 0.34 nM。在 MT-4 细胞中，用CellTiter-Glo测得的EC50 为 0.57 nM， MTT测得的EC50 为1.3 nM，在使用伪型自灭活病毒的 PHIV 测定中EC50为0.5 nM[3]。 Cell Viability Assay[3] Cell Line:
In Vivo	Cabotegravir 在小鼠中的半衰期长达 54 天[1]。 Cabotegravir (25 or 50 mg/kg; i.v.; single dose or twice) 保护 SIVmac251 对猕猴 (Macaques) 的感染[4]。
Name	Cabotegravir sodium
CAS	1051375-13-3
Formula	C19H16F2N3NaO5
Molar Mass	427.33
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Reference	[1]. Zhou T, et al. Creation of a nanoformulated cabotegravir prodrug with improved antiretroviral profiles. Biomaterials. 2018 Jan;151:53-65. [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. [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. [4]. Andrews CD, et al. Cabotegravir long acting injection protects macaques against intravenous challenge with SIVmac251. AIDS. 2017 Feb 20;31(4):461-467.