CC618 is a potent and selective PPARβ/δ antagonist. CC618 selectively antagonizes agonist-induced PPARβ/δ activity with an IC50 = 10.0 μM. The treatment of PPARβ/δ with CC618 leads to a covalent modification of Cys249, located centrally in the PPARβ/δ ligand binding pocket, corresponding to the conversion of its thiol moiety to a 5-trifluoromethyl-2-pyridylthioether.
