1680204-90-3

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.

CC618 is a selective peroxisome proliferator-activated receptor (PPARβ/δ) antagonist that exhibits antagonism by covalently binding to PPARβ/δ receptors[1].

[1] Kaupang ?, et al. Synthesis, biological evaluation and molecular modeling studies of the PPARβ/δ antagonist CC618. Eur J Med Chem. 2015 Apr 13;94:229-36. DOI:10.1016/j.ejmech.2015.03.006