Cabotegravir (GSK744, GSK1265744)

Cabotegravir (GSK744, GSK1265744) Basic information
Product Name:Cabotegravir (GSK744, GSK1265744)
Synonyms:GSK1265744;GSK744;(3S,11aR)-N-[(2,4-Difluorophenyl)methyl]-2,3,5,7,11,11a-hexahydro-6-hydroxy-3-methyl-5,7-dioxo-oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamide;Cabotegravir (GSK744, GSK1265744);Cabotegravir Free Acid;Cabotegravir;Cyclic pyranopterin;SK744, GSK1265744
CAS:1051375-10-0
MF:C19H17F2N3O5
MW:405.35
EINECS:
Product Categories:Inhibitors
Mol File:1051375-10-0.mol
Cabotegravir (GSK744, GSK1265744) Structure
Cabotegravir (GSK744, GSK1265744) Chemical Properties
Boiling point 664.0±55.0 °C(Predicted)
density 1.57±0.1 g/cm3(Predicted)
storage temp. Store at -20°C
solubility insoluble in H2O; insoluble in EtOH; ≥19.35 mg/mL in DMSO with gentle warming
form solid
pka4.50±1.00(Predicted)
Safety Information
MSDS Information
Cabotegravir (GSK744, GSK1265744) Usage And Synthesis
UsesCabotegravir is a long acting HIV-1 integrase inhibitor with action against a broad range of HIV subtypes.
DefinitionChEBI: Cabotegravir is a monocarboxylic acid amide obtained by formal condensation of the carboxy group of (3S,11aR)-6-hydroxy-3-methyl-5,7-dioxo-2,3,5,7,11,11a-hexahydro[1,3]oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxylic acid with the amino group of 2,4-difluorobenzylamine. Used (as its sodium salt) for treatment of HIV-1. It has a role as a HIV-1 integrase inhibitor. It is a difluorobenzene, a secondary carboxamide, a monocarboxylic acid amide and an organic heterotricyclic compound. It is a conjugate acid of a cabotegravir(1-).
Biological ActivityCabotegravir (GSK744, GSK1265744) is a long-acting HIV integrase inhibitor against a broad range of HIV subtypes, inhibiting HIV-1 integrase-catalyzed strand transfer with IC50 of 3 nM. Phase 2.
Mechanism of actionCaboggravir is a potent inhibitor of HIV integrase, which prevents the HIV virus from infecting human cells, while rilpivirine prevents the virus from replicating itself.
targetHIV integrase
Cabotegravir (GSK744, GSK1265744) Preparation Products And Raw materials
Elvitegravir LY 294002 HYDROCHLORIDE Lopinavir Raltegravir BMS707035 Tenofovir disoproxil fumarate

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