CAY10592

CAY10592 is a full PPARδ agonist (EC₅₀ = 30 nM) in a fatty acid oxidation assay of rat L6 muscle cells with desirable oral pharmacokinetic properties.¹ In a transactivation assay using human PPAR receptors, CAY10592 acts as a selective partial PPARδ agonist (EC₅₀ = 53 nM) with no effect on PPARα or PPARγ activity up to 30 µM.¹ Chronic treatment of high fat fed ApoB100/CETP-transgenic mice with CAY10592 at a dose of 20 mg/kg increases HDL levels, decreases LDL and TG levels, and improves insulin sensitivity.¹

WARNING This product is not for human or veterinary use.

1. Sauerberg, P., Olsen, G.S., Jeppesen, L., et al. Identification and synthesis of a novel selective partial PPARδ agonist with full efficacy on lipid metabolism in vitro and in vivo. J. Med. Chem. 50, 1495-1503 (2007).

Tiefenbach, J., Magomedova, L., Liu, J., et al. Idebenone and coenzyme Q10 are novel PPARα/γ ligands, with potential for treatment of fatty liver diseases. Dis. Model Mech. 11(9), (2018).