ASP7657 free base 

ASP7657 free base is an orally active EP4 receptor antagonist, with K_is of 2.21 and 6.02 nM for the human and rat EP4 receptors^[1].

ASP7657 free base inhibits the PGE2-induced cAMP increase in CHO cells (expressing rat EP4 receptors) and human lymphoblastoid T cells, with IC₅₀ values of 0.86 nM and 0.29 nM, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

ASP7657 free base (0.1 mg/kg, p.o., rats) shows a t_1/2 of 1.38 h, C_max of 22.4 ng/mL, and oral bioavailability of 46.2%^[1].
ASP7657 free base (0.003-0.1 mg/kg, p.o.) inhibits LPS (1 μg/mL)-induced TNF-α release from rat whole blood^[1].
ASP7657 free base (0.01 mg/kg, p.o.) attenuates urinary albumin excretion in type 2 diabetic mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

509.52

C₂₈H₂₆F₃N₃O₃

1196045-28-9

O=C([C@H]1CC[C@H](CNC(C2=CC(C(F)(F)F)=CC3=C2N(CC4=NC5=CC=CC=C5C=C4)C=C3)=O)CC1)O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Mizukami K, et al. Pharmacological properties of ASP7657, a novel, potent, and selective prostaglandin EP4 receptor antagonist. Naunyn Schmiedebergs Arch Pharmacol. 2018 Dec;391(12):1319-1326.  [Content Brief]