Bictegravir

SKU: orb1226059

Description

Bictegravir (GS 9883) is a novel potent HIV-1 integrase (IN) that specifically targets IN strand transfer activity with IC50 of 7.5 nM; exhibits potent and selective in vitro antiretroviral activity in both T-cell lines and primary human T lymphocytes with EC50 of 1.5-2.4 nM, with minimal cytotoxicity; exhibits synergistic in vitro antiviral effects in pairwise combinations with tenofovir alafenamide, emtricitabine, or darunavir and maintains potent antiviral activity against HIV-1 variants.HIV Infection Phase 3 Clinical(In Vitro):Bictegravir (BIC) 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 IN, with an IC50 of 241±51 nM. Bictegravir enhances the accumulation of 2-LTR circles ~5-fold relative to the mock-treated control and reduces the amount of authentic integration products in infected cells by 100-fold. Bictegravir potently inhibits HIV-1 replication in both MT-2 and MT-4 cells with EC50s of 1.5 and 2.4 nM, respectively. Bictegravir exhibits potent antiviral effects in both primary CD4+ T lymphocytes and monocyte-derived macrophages, with EC50s of 1.5±0.3 nM and 6.6±4.1 nM, respectively, which are comparable to values obtained in T-cell lines.

Key Properties

• CAS Number: 1611493-60-7
• MW: 449.39
• Purity: >98% (HPLC)
• Formula: C₂₁H₁₈F₃N₃O₅
• SMILES: C1CC2CC1N3C(O2)CN4C=C(C(=O)C(=C4C3=O)O)C(=O)NCC5=C(C=C(C=C5F)F)F
• Target: HIV
• Solubility: DMSO: 80 mg/mL （ < 1 mg/ml refers to the product slightly soluble or insoluble )

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GS 9883

Quick Database Links

Gene Symbol

HIV