Pioglitazone

Pioglitazone is an agonist of the peroxisome proliferator-activated receptor ? (PPAR?; EC50 = ~500-600 nM for both human and murine PPAR?).{10857,10670} It is selective for PPAR? over PPAR?, exhibiting low level activation of PPAR? at 1 µM and 5.4-fold activation at a concentration of 10 µM.{10857} Pioglitazone inhibits pyruvate oxidation and glucose production in hepatocytes when used at a concentration of 10 ?M.{37440} In vivo, pioglitazone (0.3-3 mg/kg per day) reduces hyperglycemia, hyperlipidemia, and hyperinsulinemia in a dose-dependent manner in male Wistar fatty rats.{37441} It reduces the number of lesions in a transgenic rat adenocarcinoma of prostate (TRAP) model.{37442} Pioglitazone (2.5 mg/kg) also decreases production of neuroinflammatory cytokines and reduces immobility in the forced swim and tail suspension tests in a mouse model of chronic mild stress, indicating antidepressant-like activity that can be reversed by the PPAR? antagonist GW9662 (Item No. 70785).{37443}