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Pioglitazone potassium
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Pioglitazone potassium图片
CAS NO:1266523-09-4
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
U 72107 potassium
产品介绍
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)

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].

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.
Clinical Trial
分子量

394.53

Formula

C19H19KN2O3S

CAS 号

1266523-09-4

中文名称

吡格列酮钾盐;酮基匹格列酮钾盐

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.