ST247 a potent PPARβ/δ inverse agonist. ST247 has a higher affinity to PPARβ/δ. ST247 modulates expression of the activation marker CCL2 in the opposite direction. ST247 efficiently induces the interaction with corepressors. ST247 inhibits the agonist-induced transcriptional activity of PPARβ/δ.
ST247 induces a clearly enhanced interaction of the PPARβ/δ LBD with the SMRT-ID2 peptide, with an EC50 of 10 nM[1].
ST247 down-regulates basal level expression of the peroxisome proliferator responsive element-driven PPARβ/δ target gene ANGPTL4, with an IC50 of 19.1 nM[1].
References:
[1]. Naruhn S, et al. High-affinity peroxisome proliferator-activated receptor β/δ-specific ligands with pure antagonistic or inverse agonistic properties. Mol Pharmacol. 2011 Nov;80(5):828-38.