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Cabotegravir

CAT: 0804-HY-15592-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-15592-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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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].
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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Launched

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