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

pka

4.50±1.00(Predicted)

Cabotegravir (GSK744, GSK1265744) Usage And Synthesis

Uses

Cabotegravir is a long acting HIV-1 integrase inhibitor with action against a broad range of HIV subtypes.

Definition

ChEBI: 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 Activity

Cabotegravir (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 action

Caboggravir is a potent inhibitor of HIV integrase, which prevents the HIV virus from infecting human cells, while rilpivirine prevents the virus from replicating itself.

target

HIV integrase

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