pparγ lbd leriglitazone

Leriglitazone, a metabolite of pioglitazone, binds to the PPARγ C-terminal ligand-binding domain (Ki: 1.2 μM) and induces transcriptional efficacy of the PPARγ (EC50: 680 nM). Leriglitazone PioOH is a PPARγ agonist, stabilizes the PPARγ activation functio

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].