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Boceprevir

Boceprevir

产品编号 T4988   CAS 394730-60-0
别名: SCH 503034, EBP 520, 波普瑞韦

Boceprevir 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。

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Boceprevir, CAS 394730-60-0
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产品目录号及名称: Boceprevir (T4988)
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纯度: 99.16%
纯度: 97.33%
纯度: 95%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Boceprevir is a novel, potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with Ki of 14 nM in both enzyme assay and EC90 of 350 nM in cell-based replicon assay.
靶点活性 HCV NS3 protease:14nM(Ki)
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.
别名 SCH 503034, EBP 520, 波普瑞韦
分子量 519.68
分子式 C27H45N5O5
CAS No. 394730-60-0

存储

Powder: -20°C for 3 years | In solvent: -80°C for 2 years

溶解度

DMSO: 91 mg/mL(175.1 mM)

( < 1 mg/mL refers to the product slightly soluble or insoluble )

参考文献

1. Yao M, et al. Conditional Inducible Triple-Transgenic Mouse Model for Rapid Real-Time Detection of HCV NS3/4A ProteaseActivity. PLoS One. 2016 Mar 4;11(3):e20150894. 2. Coilly A, et al. Practical management of boceprevir and immunosuppressive therapy in liver transplant recipients with hepatitis C virus recurrence. Antimicrob Agents Chemother. 2012 Nov;56(11):5728-34. 3. Burton MJ, et al. Telaprevir and boceprevir in african americans with genotype 1 chronic hepatitis C: implications for patients and providers. South Med J. 2012 Aug;105(8):431-6. 4. Njoroge FG, et al. Challenges in modern drug discovery: a case study of boceprevir, an HCV protease inhibitor for the treatment of hepatitis C virus infection. Acc Chem Res. 2008 Jan;41(1):50-9. 5. Berenguer M, et al. New developments in the management of hepatitis C virus infection: focus on boceprevir. Biologics. 2012;6:249-56. 6. Fical L. Vývoj UHPLC-MS/MS metody pro analýzu vybraných antivirotik v HILIC a RP módu[J]. 2020 7. Fical L, Khalikova M, Kočová Vlčková H, et al. Determination of Antiviral Drugs and Their Metabolites Using Micro-Solid Phase Extraction and UHPLC-MS/MS in Reversed-Phase and Hydrophilic Interaction Chromatography Modes[J]. Molecules. 2021, 26(8): 2123.

文献引用

1. Bai Y, Ye F, Feng Y, et al. Structural basis for the inhibition of the SARS-CoV-2 main protease by the anti-HCV drug narlaprevir. Signal Transduction and Targeted Therapy. 2021, 6(1): 1-3 2. Fical L, Khalikova M, Kočová Vlčková H, et al. Determination of Antiviral Drugs and Their Metabolites Using Micro-Solid Phase Extraction and UHPLC-MS/MS in Reversed-Phase and Hydrophilic Interaction Chromatography Modes. Molecules. 2021, 26(8): 2123.
Pinokalant Setrobuvir GS-443902 Grazoprevir Mizoribine Remdesivir Asunaprevir Theodrenaline hydrochloride

相关化合物库

该产品包含在如下化合物库中:
药物功能重定位化合物库 蛋白酶抑制剂库 人代谢物化合物库 肝脏毒性化合物库 抗感染化合物库 NO PAINS 化合物库 抗COVID-19化合物库 已知活性化合物库 免疫/炎症分子化合物库 经典已知活性库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% ddH2O
计算 重置

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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g/mol

输入分子式,点击计算,可计算出产品的分子量。

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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Boceprevir 394730-60-0 Microbiology/Virology Proteases/Proteasome SARS-CoV HCV Protease HCV SARS coronavirus SCH 503034 SCH-503034 SCH503034 Inhibitor Hepatitis C virus EBP520 EBP 520 EBP-520 inhibit 波普瑞韦 inhibitor

 

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