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 EC 50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone can be used in diabetes research.
性状
Solid
IC50 & Target[1][2]
hPPARγ 0.93 μM (EC50) mouse PPARγ 0.99 μM
体外研究(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.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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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.
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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Kuwabara K, et al. A novel selective peroxisome proliferator-activated receptor alpha agonist, 2-methyl-c-5-[4-[5-methyl-2-(4-methylphenyl)-4-oxazolyl]butyl]-1,3-dioxane-r-2-carboxylic acid (NS-220), potently decreases plasma triglyceride and glucose leve[2]. Puddu A, et al. Pioglitazone attenuates the detrimental effects of advanced glycation end-products in the pancreatic beta cell line HIT-T15. Regul Pept. 2012 Aug 20;177(1-3):79-84.
溶解度数据
In Vitro: DMSO : 40 mg/mL (112.22 mM; ultrasonic and warming and heat to 60°C)配制储备液