Description: | Leriglitazone (MIN-102; Hydroxypioglitazone) hydrochloride, a metabolite of pioglitazone. Leriglitazone hydrochloride PioOH is a PPAR? agonist, stabilizes the PPAR? activation function-2 (AF-2) co-activator binding surface and enhances co-activator binding, affording slightly better transcriptional efficacy. Leriglitazone hydrochloride binds to the PPAR? C-terminal ligand-binding domain (LBD) with a Ki of 1.2 ?M?Leriglitazone induces transcriptional efficacy of the PPAR? (LBD) with an EC50 of 680 nM[1]. |