Cabotegravir
Product Specifications
UNSPSC Description
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].
Target Antigen
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
Solubility
DMSO : 16.67 mg/mL (ultrasonic)
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 Weight
405.35
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.
Shipping Conditions
Room Temperature
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-15592/Cabotegravir-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-15592/Cabotegravir-SDS-MedChemExpress.pdf
Clinical Information
Launched
CAS Number
1051375-10-0
Available Sizes
Curated Selection
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