Bictegravir

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Bictegravir (GS 9883) 是一种新型有效的 HIV-1 整合酶 (IN)，专门针对 IN 链转移活性，IC50 为 7.5 nM。

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.

——

——

GS 9883

Microbiology/Virology

HIV

HIV-1integrase

Infection

HIV Infection

1611493-60-7

449.39

C21H18F3N3O5

>98% (HPLC)

DMSO: 80 mg/mL （ < 1 mg/ml refers to the product slightly soluble or insoluble )

C1CC2CC1N3C(O2)CN4C=C(C(=O)C(=C4C3=O)O)C(=O)NCC5=C(C=C(C=C5F)F)F

(2R,5S,13aR)-8-hydroxy-7,9-dioxo-N-(2,4,6-trifluorobenzyl)-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

(-20℃)

With Ice Pack

≥ 2 years