1356497-91-0

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[1].

ST247 is a PPAR β/δ selective inverse agonist. The compound is based on the structure of GSK0660and is 10-fold more potent in blocking the transcription of endogenous target genes: ST247 IC50 = 19 nm vs. GSK0660 IC50 = 210 nM.

PPARβ/δ

[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. DOI:10.1124/mol.111.074039