Bictegravir 25mg


HIV protease inhibitor

SKU: BSV-S5911-25

Bictegravir is a novel, potent, once-daily, unboosted inhibitor of HIV-1 integrase.

Target: HIV-1 integrase

Chemical name: 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]-, (2R,5S,13aR)-

Formula: C21H18F3N3O5

Molecular weight: 449.38

Size: 25 mg

Purity: 99.93 %

Solubility: 90 mg/mL (DMSO)

Storage: 3 years -20°C powder, 2 years -80°C in solvent

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[1].

[1] Tsiang M, et al. Antimicrob Agents Chemother. 2016, 60(12):7086-7097.