Name: Simeprevir
Price: 328.00 USD

- Overview
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    Background
    
    Simeprevir is a potent inhibitor of HCV NS3/4A protease with Ki value of 0.36 nM [1].The hepatitis C virus (HCV) NS3/4A protease is a serine protease encoded by HCV and is responsible for cleavage at four sites of the HCV polyprotein. It is essential for viral replication [1].In Huh-7-Rep cells, Simeprevir inhibited HCV replication with EC50 of 7.8 nM [1]. In the Huh7-Luc HCV genotype 1b replicon cell line, Simeprevir inhibited HCV replication with EC50 and EC90 values of 8 nM and 24 nM respectively in a dose dependent way [2]. In ninety-two naive, HCV genotype 1-infected patients, treatment with Simeprevir (50 or 100 mg QD) for 12 or 24 weeks and peginterferon α-2a/ribavirin (PegIFNα-2a/RBV) for 24 or 48 weeks or PegIFN α-2a/RBV for 48 weeks lonely (PR48 group), RNA reductions in the 4 week were -5.2,-5.2 and-2.9 log10IU/mL for Simeprevir 50 mg combined, 100 mg combined and PR48 groups, respectively, which suggested Simeprevir reduced HCV RNA more rapidly and substantially. Also, Simeprevir increased the virologic response rates [3].
    
    [1]. Raboisson P, de Kock H, Rosenquist A, et al. Structure-activity relationship study on a novel series of cyclopentane-containing macrocyclic inhibitors of the hepatitis C virus NS3/4A protease leading to the discovery of TMC435350. Bioorg Med Chem Lett, 2008, 18(17): 4853-4858.
    [2]. Lin TI, Lenz O, Fanning G, et al. In vitro activity and preclinical profile of TMC435350, a potent hepatitis C virus protease inhibitor. Antimicrob Agents Chemother, 2009, 53(4): 1377-1385.
    [3]. Hayashi N, Seto C, Kato M, et al. Once-daily simeprevir (TMC435) with peginterferon/ribavirin for treatment-naïve hepatitis C genotype 1-infected patients in Japan: the DRAGON study. J Gastroenterol, 2014, 49(1): 138-147.
- Properties
  - Alternative Name
    
    TMC435,TMC435350,TMC-435350,Simeprevir
    
    CAS Number
    
    923604-59-5
    
    Molecular Formula
    
    C38H47N5O7S2
    
    Molecular Weight
    
    749.96
    
    Appearance
    
    A solid
    
    Purity
    
    99.95%
    
    Solubility
    
    insoluble in H2O; insoluble in EtOH; ≥18.75 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Lee SH, Moon JS, et al. "HA1077 displays synergistic activity with daclatasvir against hepatitis C virus and suppresses the emergence of NS5A resistance-associated substitutions in mice." Sci Rep. 2018 Aug 20;8(1):12469. PMID:30127498

Simeprevir

Simeprevir

Background

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