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首页-小分子抑制剂&激动剂-Antibiotics and Antivirals-HCV-Faldaprevir
Faldaprevir

Chemical Structure : Faldaprevir

CAS No.: 801283-95-4

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Faldaprevir (BI 201335, BI-201335)

货号: PC-60953Not For Human Use, Lab Use Only.

Faldaprevir (BI-201335) is a potent, selective noncovalent competitive inhibitor of HCV NS3/4A protease with Ki of 2.6 and 2.0 nM for GT1a and 1b NS3-NS4A protease, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    Faldaprevir (BI-201335) is a potent, selective noncovalent competitive inhibitor of HCV NS3/4A protease with Ki of 2.6 and 2.0 nM for GT1a and 1b NS3-NS4A protease, respectively.
    Faldaprevir (BI-201335) also shows Ki of 2 to 230 nM for HCV GT2 to 6, potently inhibits HCV RNA replication in vitro of 6.5 and 3.1 nM in genotype 1a and 1b replicon assays, respectively.
    Faldaprevir (BI-201335) possesses good ADME profile in vitro and pharmacokinetics in vivo.

    物理化学性质&存储条件

    分子量 869.829
    分子式 C40H49BrN6O9S
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20 °C 12 个月; 4°C 6 个月
    配置液
    -80 °C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO
    Chemical Name/SMILES

    (1R,2S)-1-[[(2S,4R)-4-[8-bromo-7-methoxy-2-[2-(2-methylpropanoylamino)-1,3-thiazol-4-yl]quinolin-4-yl]oxy-1-[(2S)-2-(cyclopentyloxycarbonylamino)-3,3-dimethylbutanoyl]pyrrolidine-2-carbonyl]amino]-2-ethenylcyclopropane-1-carboxylic acid

    参考文献

    1. Llinàs-Brunet M, et al. J Med Chem. 2010 Sep 9;53(17):6466-76.

    2. White PW, et al. Antimicrob Agents Chemother. 2010 Nov;54(11):4611-8.

    3. Manns MP, et al. J Hepatol. 2011 Jun;54(6):1114-22.

    4. Zeuzem S, et al. Gastroenterology. 2011 Dec;141(6):2047-55; quiz e14.

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