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CAS No. : 394730-60-0
MCE 国际站:Boceprevir
产品活性:Boceprevir (EBP 520) 是一种口服有效的选择性的 HCV NS3 protease 抑制剂,酶实验中Ki 为 14 nM,在含细胞体系的复制实验中,EC90 为 350 nM。Boceprevir 抑制 SARS-CoV-2 3CLpro 活性。
研究领域:Anti-infection | Metabolic Enzyme/Protease
作用靶点:HCV Protease | HCV | SARS-CoV
In Vitro: In the HCV NS3 protease continuous assay, Boceprevir (SCH 503034) has a potency of 14 nM (Ki) average over a large number of runs. In the 72-h bicistronic subgenomic cell-based replicon assay in HuH-7 cells, the EC50 and EC90 values are determined to be 0.20 µM and 0.35 µM, respectively. Boceprevir is also found to be a very weak inhibitor of HNE (Ki=26 µM) representing a selectivity of 2200.
In Vivo: Boceprevir, an HCV Protease Inhibitor for the Treatment of Hepatitis C Virus Infection. The pharmacokinetic profile of Boceprevir is evaluated in several animal species. Following oral administration, Boceprevir is moderately absorbed in rats (10 mg/kg), dogs (3 mg/kg), and monkeys (3 mg/kg). Absorption is relatively rapid in dogs but slower in mice (10 mg/kg), rats, and monkeys, as evidenced by mean absorption times (MAT) ranging from 0.5 to 1.4 h. The AUC is good in dogs and rats, moderate in mouse, and low in monkeys. The absolute oral bioavailability is modest in mouse, rats, and dogs (26-34%) but low in monkeys (4%). Boceprevir (100 mg/kg, orally) inhibit HCV NS3/4A protease activity in triple-transgenic mice.
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