Pioglitazone potassium (U 72107) is an orally active and selective agonist of peroxisome proliferator-activated receptor gamma (PPARγ). It demonstrates high affinity binding to the ligand-binding domain of PPARγ, with an EC50 of 0.93 μM and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone potassium has applications in diabetes research [2] [3] [4].

Pioglitazone potassium (0.5 or 1 μM, 5 days) can completely prevent AGEs (advanced glycation end-products)-induced β-cell necrosis and the increase of caspase-3 thereby avoiding the impaired viability caused by AGEs in pancreatic beta cell line HIT-T15 [2]. Pioglitazone potassium (1 μM, 1 h) can stimulate insulin secretion induced by low glucose concentration and attenuate the GSSG/GSH ratio in cells cultured with AGEs [2].

Pioglitazone potassium (oral gavage, 10 or 30 mg/kg, once daily, 14 days) can induce improvements in insulin resistance and diabetes that may be lipocalin-dependent in the liver but not in skeletal muscle [3]. Pioglitazone potassium (oral gavage, 10 mg/kg, once daily, 4 weeks) can significantly reduce body weight (BW), cardiac hypertrophy, elevated blood glucose levels and improve the associated dyslipidemia [4]. Animal Model: ob/ob and adipo -/- ob/ob mice with a C57Bl/6 background [3] Dosage: 10 or 30 mg/kg Administration: Oral gavage; once daily; 14 days Result: Showed no changes of serum-free fatty acid and triglyceride levels as well as adipocyte sizes in ob/ob and adipo -/- ob/ob C57BL/6 mice at 10 mg/kg but significantly reduced to a similar degree at 30 mg/kg. Also showed no changes of expressions of TNFα and resistin in adipose tissues of ob/ob and adipo -/- ob/ob mice at 10 mg/kg but decreased at 30 mg/kg. Animal Model: Male Wistar albino rats [4] Dosage: 10 mg/kg Administration: Oral gavage; once daily; 4 weeks Result: Decreased the elevated serum levels of both creatinine and creatine kinase-MB (CK-MB), TGF-β1 gene expression and regulated the expression of MMP-2/TIMP-2 system.