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Boceprevir

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基本信息:

  • 发布时间: 2017-06-12
  • 产品名称: Boceprevir
  • 产品英文名称: Boceprevir
  • CAS号: 394730-60-0
  • 产品包装: 10mg
  • 产品价格: 2000元/罐
  • 有效期: 一年

产品图片:

Boceprevir

产品描述:

Boceprevir的生物活性

 

Boceprevir(EBP-520, SCH503034) is an HCV protease inhibitor (Ki=14 nM) for the treatment of hepatitis C virus infection.
IC50 Value: 14 nM (Ki)
Target: HCV
Boceprevir is a potent inhibitor in both enzyme assay (Ki* = 14 nM) and cell-based replicon assay (EC 90 = 0.35 microM). It is highly selective (2200x) against human neutrophil elastase (HNE). Boceprevir is well tolerated in humans and demonstrated antiviral activity in phase I clinical trials. It is currently in phase II trials. This Account details the complexity and challenges encountered in the drug discovery process.
Treatment with Boceprevir triple therapy increased SVR to 63-66% compared to 38% receiving PEG-IFN/RBV therapy. Non-Black patients achieved higher SVR rates compared to Black patients. Responsiveness to interferon in the lead-in phase was predictive for SVR. SVR rates did not differ between patients randomized to RGT with Boceprevir and those treated with a fixed duration. Anaemia was the most important adverse event leading to dose reduction of RBV in 13% of controls and 21% of Boceprevir recipients.

 

化学信息

分子量
519.68
储存条件
参考CoA中推荐的条件进行储存。
分子式
C27H45N5O5
CAS号
394730-60-0
溶剂/溶解度
10 mM in DMSO

 

相关文献

 

[1]. Degertekin B, Lok AS (May 2008). Update on viral hepatitis: 2007. Curr. Opin. Gastroenterol. 24 (3): 306–11.

[2]. Njoroge FG, Chen KX, Shih NY, Piwinski JJ (January 2008). 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. 41 (1): 50–9.

[3]. Coilly A, Furlan V, Roche B, Barau C, No?l C, Bonhomme-Faivre L, Antonini TM, Roque-Afonso AM, Samuel D, Taburet AM, Duclos-Vallée JC.PRACTICAL MANAGEMENT OF BOCEPREVIR AND IMMUNOSUPPRESSIVE THERAPY IN LIVER TRANSPLANT RECIPIENTS WITH HEPATITIS C VIRUS RECURRENCE.Antimicrob Agents Chemother. 2012 Aug 20.

[4]. Berenguer M, López-Labrador FX.New developments in the management of hepatitis C virus infection: focus on boceprevir.Biologics. 2012;6:249-56. Epub 2012 Aug 3.

[5]. Burton MJ, Passarella MJ, McGuire BM.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.

  • 供应商联系方式:
  • 联系人 谢小姐
  • 公司名称 深圳市浩博世纪生物有限公司
  • 电话 0755-29573896
  • 手机 15994704873
  • 传真 
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