ASP7657

Research use only, not for human use.

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 (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; 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; 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-α release from rat whole blood culture, attenuates albuminuria in type 2 diabetic mice at dose of 0.1 mg/kg.Diabetes Phase 1 Discontinued.

——

Animal Model:LPS (1 μg/mL)-induced ratsDosage:0.003, 0.01, 0.03, 0.1 mg/kg Administration:p.o.Result:Antagonized the PGE2-mediated inhibition of LPS-induced TNF-α release from rat whole blood culture, in a dose-dependent way.

ASP 7657 | ASP-7657

GPCR/G Protein

Prostaglandin Receptor

Prostaglandin Receptor

Metabolic Disease

Diabetes

1196045-28-9

509.529

C28H26F3N3O3

>98% (HPLC)

——

FC(F)(F)C1=CC2=CC[N](CC(C=C3)=NC4=C3C=CC=C4)=C2C(C([N]C[C@@H]5CC[C@@H](C([O])=O)CC5)=O)=C1

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

(-20℃)

With Ice Pack

≥ 2 years