Pioglitazone

Pioglitazone (U 72107) is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC₅₀ of 0.93 and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone can be used in diabetes research^[2][3][4]. IC50 & Target:EC50: 0.93 μM (human PPARγ), 0.99 μM (mouse PPARγ)^[1] In Vitro: Pioglitazone (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 (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].
In Vivo: Pioglitazone (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 (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].