产品
编 号:F038198
分子式:C19H20N2O3S
分子量:356.44
产品类型
结构图
CAS No: 111025-46-8
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产品详情
生物活性:
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.
体内研究:
Pioglitazone (口服,10 或 30 mg/kg,每天一次,14 天) 可改善胰岛素抵抗和糖尿病,这可能在肝脏中依赖脂质运载蛋白,但在骨骼肌中不依赖。Pioglitazone (口服灌胃,10 mg/kg,每日一次,4 周) 可显著减轻体重 (BW)、心肌肥厚、血糖水平升高并改善相关的血脂异常。Animal Model:ob/ob and adipo-/- ob/ob mice with a C57Bl/6 background
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
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.
体外研究:
Pioglitazone (0.5 或 1 μM,5 天) 可完全阻止 AGEs (晚期糖基化终产物) 诱导的 β 细胞坏死和 caspase-3 的增加,从而避免 AGEs 导致的胰腺 β 细胞系 HIT-T15 的活力受损。Pioglitazone (1 μM,1 h) 可刺激低葡萄糖浓度诱导的胰岛素分泌,并降低 AGEs 培养细胞中的 GSSG/GSH 比值。