中文名:Bictegravir
英文名:Bictegravir
纯度:Moligand™,≥99%
货号:B413365
Cas号:1611493-60-7
存储温度:-20°C储存
运输条件:超低温运输
产品介绍:
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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