Leriglitazone

Description: Leriglitazone, a metabolite of pioglitazone, binds to the PPARgamma C-terminal ligand-binding domain (Ki: 1.2 µM) and induces transcriptional efficacy of the PPARgamma (EC50: 680 nM). Leriglitazone PioOH is a PPARgamma agonist, stabilizes the PPARgamma activation function-2 (AF-2) co-activator binding surface. Target: Others. Smiles: O=C1SC(C(=O)N1)CC2=CC=C(OCCC3=NC=C(C=C3)C(O)C)C=C2. References: Mosure SA,et al. Structural Basis of Altered Potency and Efficacy Displayed by a Major in Vivo Metabolite of the Antidiabetic PPARgamma Drug Pioglitazone. J Med Chem. 2019 Feb 28,62(4):2008-2023.