波普瑞韦 T4988

Product Introduction
Bioactivity


英文名: Boceprevir

描述: Boceprevir (SCH 503034) 是一种口服有效的选择性 HCV NS3 蛋白酶抑制剂。在酶试验中的 Ki 为 14 nM，在基于细胞的复制子试验中 EC90 为 350 nM。它也是 SARS-CoV-2 3CLpro 抑制剂。

体外活性: 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.

体内活性: Boceprevir is an HCV Protease Inhibitor for the Treatment of Hepatitis C Virus Infection. The pharmacokinetic profile of Boceprevir is evaluated in several animal species. Boceprevir is moderately absorbed in rats (10 mg/kg), dogs (3 mg/kg), and monkeys (3 mg/kg) following oral administration. 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%)[1]. Boceprevir (100 mg/kg, orally) inhibit HCV NS3/4A protease activity in triple-transgenic mice.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 91 mg/mL(175.1 mM)


关键字: HCV | SARS-CoV | SARS coronavirus | HCV Protease | Inhibitor | Hepatitis C virus | Boceprevir | EBP520 | SCH503034 | inhibit | SCH-503034 | EBP-520

相关产品: Grazoprevir | Voxilaprevir | Mulberroside C | MK-0608 | Sovaprevir | Paritaprevir | BLT-1 | Danoprevir | Peretinoin | Sennidin B

相关库: Anti-Aging Compound Library | Drug Repurposing Compound Library | Approved Drug Library | Clinical Compound Library | Bioactive Compounds Library Max | Inhibitor Library | EMA Approved Drug Library | Anti-Viral Compound Library | NO PAINS Compound Library | Anti-Infection Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途