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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Factor Xa-ZED3197
ZED3197

Chemical Structure : ZED3197

CAS No.: 2379345-24-9

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ZED3197 (ZED-3197)

货号: PC-72148Not For Human Use, Lab Use Only.

ZED3197 (ZED-3197) is a novel peptidomimetic direct-acting, potent and selective inhibitor of human FXIIIa, inhibits human plasma derived FXIII‐A2B2 and the recombinant cellular form (FXIII‐A2) with IC50 of 10 and 14 nM, respectively.

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

    生物&药学活性

    ZED3197 (ZED-3197) is a novel peptidomimetic direct-acting, potent and selective inhibitor of human FXIIIa, inhibits human plasma derived FXIII‐A2B2 and the recombinant cellular form (FXIII‐A2) with IC50 of 10 and 14 nM, respectively.
    ZED3197 strongly blocks FXIII‐A2 from mouse, rat, rabbit, dog, and cynomolgus monkey (IC50 8-30 nM), is a significantly weaker inhibitor of FXIII‐A2 from pig (IC50=220 nM).
    ZED3197 displays 20‐fold to 3000‐fold selectivity against human transglutaminases TG1, TG2, TG3, and TG7.
    ZED3197 prolonged clot formation, reduced clot firmness, and facilitated clot lysis in whole human blood without affecting the clotting time, indicating minimal impact on hemostasis.
    ZED3197 effectively decreased the weight of clots and facilitated flow restoration without prolongation of the bleeding time in vivo.

    物理化学性质&存储条件

    分子量 837.972
    分子式 C42H59N7O11
    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

    4-(((S,Z)-1-(((S)-1-((R)-2-(((S)-2-(((S)-2-amino-1-cyclohexyl-2-oxoethyl)amino)-1-cyclohexyl-2-oxoethyl)carbamoyl)-4-oxopyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)-7-methoxy-1,7-dioxohept-5-en-2-yl)carbamoyl)nicotinic acid

    参考文献

    1. Ralf Pasternack, et al. J Thromb Haemost. 2020 Jan;18(1):191-200.

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