Pioglitazone HCl | PPAR gamma agonist

Pioglitazone (112529-15-4) is a clinically useful antidiabetic drug.¹ It is a selective agonist of the human peroxisome proliferator-activated receptor γ 1 (PPARγ1; EC₅₀ = 490 nM², 550 nM³) with weak agonist activity at PPARα and no activity at PPARδ.²  Inhibits mitochondrial pyruvate metabolism and glucose production in hepatocytes.⁴ Suppresses production of inflammatory cytokines and shows antidepressant-like activity in mouse models.⁵

References/Citations
1) Merck 14:7452
2) Sakamoto et al. (2000), Activation of human peroxisome proliferator-activated receptor (PPAR) subtypes by pioglitazone; Biochem. Biophys. Res. Commun., 278 704
3) Wilson et al. (2000), The PPARs: From Orphan Receptors to Drug Discovery; J. Med. Chem., 43 527
4) Shannon et al. (2017), Pioglitazone Inhibits Mitochondrial Pyruvate Metabolism and Glucose Production in Hepatocytes; FEBS J., 284 451
5) Zhao et al. (2016), The Antidepressant-Like Effects of Pioglitazone in a Chronic Mild Stress Mouse Model Are Associated With PPARγ-Mediated Alteration of Microglial Activation Phenotypes; Neuroinflamm., 13 259