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ASP7657

Chemical Structure : ASP7657

CAS No.: 1196045-28-9

ASP7657 (ASP 7657;ASP-7657)

Catalog No.: 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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    Biological Activity

    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.

    Physicochemical Properties

    M.Wt 509.529
    Formula C28H26F3N3O3
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20 °C 12 Months; 4°C 6 Months
    In Solvent
    -80 °C 6 Months; -20°C 6 Months
    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

    References

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

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