Pioglitazone (potassium salt)

Pioglitazone is an agonist of the peroxisome proliferator-activated receptor γ (PPARγ; EC₅₀ = ~500-600 nM for both human and murine PPARγ).^1,2 It is selective for PPARγ over PPARα, exhibiting low level activation of PPARα at 1 µM and 5.4-fold activation at a concentration of 10 µM.¹ Pioglitazone inhibits pyruvate oxidation and glucose production in hepatocytes when used at a concentration of 10 μM.³ 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.⁴ It reduces the number of lesions in a transgenic rat adenocarcinoma of prostate (TRAP) model.⁵ 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 PPARγ antagonist GW9662 (Item No. 70785).⁶

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1. Sakamoto, J., Kimura, H., Moriyama, S., et al. Activation of human peroxisome proliferator-activated receptor (PPAR) subtypes by pioglitazone. Biochem. Biophys. Res. Commun. 278(3), 704-711 (2000).

2. Willson, T.M., Brown, P.J., Sternbach, D.D., et al. The PPARs: From orphan receptors to drug discovery. J. Med. Chem. 43(4), 527-550 (2000).

3. Shannon, C.E., Daniele, G., Galindo, C., et al. Pioglitazone inhibits mitochondrial pyruvate metabolism and glucose production in hepatocytes. FEBS J. 284(3), 451-465 (2017).

4. Sugiyama, Y., Taketomi, S., Shimura, Y., et al. Effects of pioglitazone on glucose and lipid metabolism in Wistar fatty rats. Arzneimittelforschung. 40(3), 263-267 (1990).

5. Suzuki, S., Mori, Y., Nagano, A., et al. Pioglitazone, a peroxisome proliferator-activated receptor γ agonist, suppresses rat prostate carcinogenesis. Int. J. Mol. Sci. 17(12), pii: E2071 (2016).

6. Zhao, Q., Wu, X., Yan, S., et al. The antidepressant-like effects of pioglitazone in a chronic mild stress mouse model are associated with PPARγ-mediated alteration of microglial activation phenotypes. J. Neuroinflammation 13(1), 259 (2016).