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Cabotegravir

Names

[ CAS No. ]:
1051375-10-0

[ Name ]:
Cabotegravir

[Synonym ]:
(3S,11aR)-N-(2,4-Difluorobenzyl)-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-carboxamide
Cabotegravir
Oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamide, N-[(2,4-difluorophenyl)methyl]-2,3,5,7,11,11a-hexahydro-6-hydroxy-3-methyl-5,7-dioxo-, (3S,11aR)-
GSK1265744A
unii-hmh0132z1q

Biological Activity

[Description]:

Cabotegravir is a potent HIV integrase inhibitor as an oral lead-in tablet and long-acting injectable for the treatment and prevention of HIV infection. Cabotegravir is an inhibitor of OAT1 (IC50 0.81 μM) and OAT3 (IC50 0.41 μM).IC50 value: 0.81 μM (OAT1), 0.41 μM (OAT3) [1]Target: OAT1, OAT3Cabotegravir is a potent HIV integrase inhibitor in clinical development as an oral lead-in tablet and long-acting injectable for the treatment and prevention of HIV infection.[2] Cabotegravir is an HIV-1 integrase inhibitor under development as a tablet for both oral lead-in therapy and long-acting (LA) injectable for intramuscular dosing.[3]

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> HIV Integrase
Signaling Pathways >> Anti-infection >> HIV
Research Areas >> Infection

[References]

[1]. Reese MJ, 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]. 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.

[3]. Bowers GD, Disposition and metabolism of cabotegravir: a comparison of biotransformation and excretion between different species and routes of administration in humans. Xenobiotica. 2015 Jul 1:1-16.


[Related Small Molecules]

Cenicriviroc | Ebselen | Triciribine | Raltegravir (potassium salt) | Tipranavir | DELAVIRDINE MESYLATE | Bictegravir | TAK-779 | Betulinic acid | Nelfinavir mesylate | nevirapine | Zidovudine | Celgosivir (hydrochloride) | Doravirine

Chemical & Physical Properties

[ Density]:
1.6±0.1 g/cm3

[ Boiling Point ]:
664.0±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C19H17F2N3O5

[ Molecular Weight ]:
405.352

[ Flash Point ]:
355.4±31.5 °C

[ Exact Mass ]:
405.113617

[ PSA ]:
104.36000

[ LogP ]:
-1.70

[ Vapour Pressure ]:
0.0±2.1 mmHg at 25°C

[ Index of Refraction ]:
1.661

[ Storage condition ]:
-20℃

Related Compounds