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PT-S58 is a PPAR β/δ full antagonist, and a derivative of GSK0660. PT-S58 has a three-fold higher affinity for the receptor than GSK0660 and is a potent inhibitor of agonist-induced target gene expression. PT-S58 are effective on PPRE-independent functions of PPARβ/δ. Unlike GSK0660, PT-S58 blocks the recruitment co-repressor molecules such as SMRT.