CAY10580 is a potent and selective prostaglandin EP4 receptor agonist (K i = 35 nM).

EP1 receptor:>3000 nM (Ki), EP3 receptor:2000 nM (Ki), EP2 receptor:3000 nM (Ki), EP4 receptor:35 nM (Ki)

CAY10580, at concentrations ranging from 10 to 10,000 nM and administered for 40 minutes, significantly enhances the presence of AQP2 on the apical membrane in MDCK cells, particularly at concentrations from 100 to 10,000 nM[2].

CAY10580, administered intraperitoneally at a dosage of 200 μg/kg body weight daily for three weeks, effectively combats diet-induced hypercholesterolemia, promotes endogenous bile acid synthesis, and increases their excretion in feces. In a study using six-week-old male EP4 +/+ mice challenged with a high-fat diet, these mice exhibited a 28.5% reduction in total cholesterol levels compared to the control group, with levels decreasing from 137.4 to 98.2 mg/dl, thereby nearly normalizing plasma cholesterol concentrations.