Pioglitazone (U 72107) potassium 是一种具有口服活性的选择性PPARγ(peroxisome proliferator-activated receptor) 激动剂，高亲和力结合到 PPARγ 配体结合域，作用于人和鼠 PPARγ 的EC50分别为 0.93 μM 和 0.99 μM。Pioglitazone potassium 可用于糖尿病研究。
| 生物活性 | Pioglitazone (U 72107) potassium is an orally active and selectivePPARγ(peroxisome proliferator-activated receptor) agonist with high affinity binding to thePPARγligand-binding domain withEC50of 0.93 μM and 0.99 μM for human and mousePPARγ, respectively. Pioglitazone potassium can be used in diabetes research[2][3][4]. |
| IC50& Target[1] | mouse PPARγ 0.99 μM (EC50) | h-PPARγ 0.93 μM (EC50) | hPPARδ 43 μM (EC50) | hPPARα 100 μM (EC50) | mouse PPARα 100 μM (EC50) |
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体外研究
(In Vitro) | 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].
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体内研究
(In Vivo) | 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 andadipo-/-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 andadipo-/-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 andadipo-/-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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
