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Leriglitazone is a brain barrier-permeable, orally active PPARγ agonist (EC50=9 μM) and mitochondrial function modulator with neuroprotective, anti-inflammatory, and antioxidant properties for neurodegenerative disease research.

Leriglitazone (Hydroxypioglitazone) hydrochloride, a pioglitazone metabolite, acts as a PPARγ agonist, effectively stabilizing the PPARγ activation function-2 (AF-2) co-activator binding surface to enhance co-activator binding, which results in a modest improvement in transcriptional efficacy. It binds to the PPARγ C-terminal ligand-binding domain (LBD) with a dissociation constant (K i) of 1.2 μM and demonstrates transcriptional efficacy with an effective concentration (EC 50) of 680 nM [1].