CAY10592 is a peroxisome proliferator-activated receptor (PPAR) β agonist. PPARs are ligand-activated nuclear transcription factors involved in the regulation of energy homeostasis as well as insulin sensitivity and glucose metabolism . Pharmacologies of PPARβ receptor agonists, though relatively unknown, have recently been reported to elevate lower plasma triglyceride (TG) and high-density lipoprotein (HDL) cholesterol levels. CAY10592 is a full PPARβ agonist (EC50 = 30 nM) in a fatty acid oxidation assay of rat L6 muscle cells. In a transactivation assay using human PPAR receptors, CAY10592 acts as a selective partial PPARβ agonist (EC50 = 53 nM) with no effect on PPARγ or PPARα activity up to 30 M.
