Bictegravir Sodium

Names

[ Name ]:
Bictegravir Sodium

[Synonym ]:
GS-9883-01
(2R,5S,13aR)-8-hydroxy-7,9-dioxo-N-[(2,4,6-trifluorophenyl)methyl]-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide monosodium salt
4L5MP1Y7W7
Bictegravir sodium
2,5-Methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide, 2,3,4,5,7,9,13,13a-octahydro-8-hydroxy-7,9-dioxo-N-[(2,4,6-trifluorophenyl)methyl]-, sodium salt, (2R,5S,13aR)- (1:1)
GS-9883
Sodium (1S,11R,13R)-3,6-dioxo-7-[(2,4,6-trifluorobenzyl)carbamoyl]-12-oxa-2,9-diazatetracyclo[11.2.1.02,11.04,9]hexadeca-4,7-dien-5-olate
UNII:4L5MP1Y7W7

Biological Activity

[Description]:

Bictegravir sodium is a potent inhibitor of HIV-1 integrase, with an IC50 of 7.5 nM. Bictegravir sodium exhibits potent and selective anti-HIV activity and low cytotoxicity[1].

[Related Catalog]:

Signaling Pathways >> Anti-infection >> HIV

Research Areas >> Infection

Signaling Pathways >> Metabolic Enzyme/Protease >> HIV Integrase

[Target]

HIV-1

[In Vitro]

Bictegravir sodium potently inhibits HIV-1 replication in both MT-2 and MT-4 cells with EC50s of 1.5 and 2.4 nM, respectively, and selectivity indices (50% cytotoxic concentration [CC50]/EC50) of ∼6,800 in MT-2 cells and ∼1,500 in MT-4 cells[1].

[References]

[1]. Tsiang M, et al. Antiviral Activity of Bictegravir (GS-9883), a Novel Potent HIV-1 Integrase Strand Transfer Inhibitor with an Improved Resistance Profile. Antimicrob Agents Chemother. 2016 Nov 21;60(12):7086-7097.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₁H₁₇F₃N₃NaO₅

[ Molecular Weight ]:
471.362

[ Exact Mass ]:
471.101807

[ Storage condition ]:
-20°C

Related Compounds

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