Bictegravir - 99%, high purity , Human immunodeficiency virus type 1 integrase inhibitor, CAS No.1611493-60-7, Human immunodeficiency virus type 1 integrase inhibitor

Item Number

B413365

• Synonyms: 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,
• Specifications & Purity: Moligand™, ≥99%
• Biochemical and Physiological Mechanisms: Bictegravir (GS-9883) is a novel, potent, once-daily, unboosted inhibitor of HIV-1 integrase.
• Storage Temp: Store at -20°C
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™
• Action Type: INHIBITOR
• Mechanism of action: Human immunodeficiency virus type 1 integrase inhibitor

Product Description

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.