Information Bictegravir (GS-9883) is a novel, potent, once-daily, unboosted inhibitor ofHIV-1 integrase. Targets HIV-1 integrase In vitro Bictegravir exhibits potent and selective in vitro antiretroviral activity in both T-cell lines and primary human T lymphocytes, with 50% effective concentrations ranging from 1.5 to 2.4 nM and selectivity indices up to 8,700 relative to cytotoxicity. Bictegravir inhibits the strand transfer activity with an IC50 of 7.5 ± 0.3 nM. Relative to its inhibition of strand transfer activity, Bictegravir is a much weaker inhibitor of 3\'-processing activity of HIV-1 integrase, with an IC50 of 241 ± 51 nM. Bictegravir 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.
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Bictegravir
CAS number：1611493-60-7 molecular formula：C21H18F3N3O5
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| Chinese alias | 比克替拉韦 | ||
| English alias | F0921-1055 | 1611493-60-7 | D10909 | 8GB79LOJ07 | BCP25703 | GS 9883 | J-517791 | SOLUWJRYJLAZCX-LYOVBCGYSA-N | Bictegravir [INN] | BICTEGRAVIR [USAN] | bictegravirum | BICTEGRAVIR [WHO-DD] | (2R,5S,13aR)-8-hydroxy-7,9-dioxo-N-(2,4,6-trifluorobenzyl)-2,3, | ||
| CAS number | 1611493-60-7 | molecular formula | C21H18F3N3O5 |
| molecular weight | 449.38 g/mol | Exact mass | - |
| PSA | 99.200 Ų | logp | 2.7 |
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