Boceprevir-d9(Synonyms: EBP 520-d9; SCH 503034-d9)

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Boceprevir-d9 (Synonyms: EBP 520-d9; SCH 503034-d9)

Boceprevir-d9 (EBP 520-d9) 是 Boceprevir 的氘代物。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。

Boceprevir-d9(Synonyms: EBP 520-d9; SCH 503034-d9)

Boceprevir-d9 Chemical Structure

CAS No. : 1256751-11-7

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生物活性

Boceprevir-d9 (EBP 520-d9) is the deuterium labeled Boceprevir. Boceprevir (EBP 520) is a potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with a Ki of 14 nM in both enzyme assay and an EC90 of 350 nM in cell-based replicon assay[1][2][3][4][5]. Boceprevir inhibits SARS-CoV-2 3CLpro activity[6].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

528.73

Formula

C27H36D9N5O5
CAS 号

1256751-11-7
中文名称

波普瑞韦 d9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. 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.

    [3]. 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):e0150894.

    [4]. 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.

    [5]. Berenguer M, et al. New developments in the management of hepatitis C virus infection: focus on boceprevir. Biologics. 2012;6:249-56.

    [6]. 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.

    [7]. Qi Sun, et al. Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. Signal Transduct Target Ther. 2021 May 29;6(1):212.

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