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首页-小分子抑制剂&激动剂-GPCR-Prostaglandin Receptor-ASP7657
ASP7657

Chemical Structure : ASP7657

CAS No.: 1196045-28-9

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ASP7657 (ASP 7657;ASP-7657)

货号: PC-35542Not For Human Use, Lab Use Only.

ASP7657 (ASP-7657) is a potent, selective, orally active prostaglandin EP4 receptor antagonist with Ki values of 6.02 nM and 2.21 nM for rat and human EP4 receptors, resepctively.

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

    生物&药学活性

    ASP7657 (ASP-7657) is a potent, selective, orally active prostaglandin EP4 receptor antagonist with Ki values of 6.02 nM and 2.21 nM for rat and human EP4 receptors, resepctively.
    ASP7657 potently inhibits the PGE2-induced cAMP increase in CHO cells expressing rat EP4 receptors and human lymphoblastoid T (Jurkat) cells, with IC50 values of 0.86 nM and 0.29 nM, respectively.
    ASP7657 does not inhibit the PGE2-induced intracellular calcium increase in HEK293 cells expressing rat EP1 and EP3 receptors, or cAMP increase in CHO cells expressing rat EP2 receptors.
    ASP7657 dose-dependently inhibits the PGE2-mediated inhibition of LPS-induced TNF-α release from rat whole blood culture, attenuates albuminuria in type 2 diabetic mice at dose of 0.1 mg/kg.

    物理化学性质&存储条件

    分子量 509.529
    分子式 C28H26F3N3O3
    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,4r)-4-((1-(quinolin-2-ylmethyl)-5-(trifluoromethyl)-1H-indole-7-carboxamido)methyl)cyclohexane-1-carboxylic acid

    参考文献

    1. Mizukami K, et al. Naunyn Schmiedebergs Arch Pharmacol. 2018 Aug 3. doi: 10.1007/s00210-018-1545-x.

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