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Cabotegravir

Chemical Structure : Cabotegravir

CAS No.: 1051375-10-0

Cabotegravir (GSK-1265744, GSK1265744, GSK744)

Catalog No.: PC-21806Not For Human Use, Lab Use Only.

Cabotegravir (GSK-1265744) is a potent, selective HIV-1 integrase inhibitor with IC50 of 3 nM in biochemical integrase strand transfer assay (INST).

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Biological Activity

Cabotegravir (GSK-1265744) is a potent, selective HIV-1 integrase inhibitor with IC50 of 3 nM in biochemical integrase strand transfer assay (INST).
Cabotegravir (GSK-1265744) shows IC50 of 1.3 nM in MT-4 cell assays, and a pHIV IC50 of <2 nM against the Q148K variant, IC50 of 0.2 nM in peripheral blood mononuclear cell (PBMC) HIV multiround replication assays.
Cabotegravir (GSK-1265744) formulated as a long-acting (LA) injectable protects macaques from intrarectal simian/human immunodeficiency virus.

Physicochemical Properties

M.Wt 405.36
Formula C19H17F2N3O5
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(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

References

1. Johns BA, et al. J Med Chem. 2013 Jul 25;56(14):5901-16.

2. Andrews CD, et al. Science. 2014 Mar 7;343(6175):1151-4.

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