Description
ASP7657 (ASP-7657) is a potent, selective, orally active prostaglandin EP4 receptor antagonist with Ki values of 6.02nM and 2.21nM for rat and human EP4 receptors, resepctively; potently inhibits the PGE2-induced cAMP increase in CHO cells expressing rat EP4 receptors and human lymphoblastoid T (Jurkat) cells, with IC50 values of 0.86nM and 0.29nM, respectively; 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; dose-dependently inhibits the PGE2-mediated inhibition of LPS-induced TNF-alpha release from rat whole blood culture, attenuates albuminuria in type 2 diabetic mice at dose of 0.1mg/kg. Diabetes Phase 1 Discontinued