Cabotegravir

Cabotegravir (GSK-1265744) 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 is primarily metabolized by uridine diphosphate glucuronosyltransferase (UGT) 1A1, with low potential to interact with other antiretroviral agents (ARVs) . Cabotegravir can be used to research AIDS[1][2].

Product Specifications

CAS Number

[1051375-10-0]

Product Name Alternative

GSK-1265744; S/GSK1265744

UNSPSC

12352005

Hazard Statement

H303, H320

Target

HIV; HIV Integrase; OAT

Type

Reference compound

Related Pathways

Anti-infection; Membrane Transporter/Ion Channel; Metabolic Enzyme/Protease

Applications

COVID-19-anti-virus

Field of Research

Infection

Assay Protocol

https://www.medchemexpress.com/Cabotegravir.html

Concentration

10mM

Purity

99.91

Solubility

DMSO : 14 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

FC1=C(CNC(C2=CN3C(C(N([C@@H](C)CO4)[C@@]4([H])C3)=O)=C(O)C2=O)=O)C=CC(F)=C1

Molecular Formula

C19H17F2N3O5

Molecular Weight

405.35

Precautions

H303, H320

References & Citations

[1]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. 2015 Sep 4:1-12.|[2]Zhou T, et al. Creation of a nanoformulated cabotegravir prodrug with improved antiretroviral profiles. Biomaterials. 2018 Jan;151:53-65.|[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.