Ciglitazone(Synonyms: 环格列酮; ADD-3878; U-63287)

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Ciglitazone (Synonyms: 环格列酮; ADD-3878; U-63287)

Ciglitazone 是一种有效的选择性 PPARγ 激动剂 (EC50=3 μM)。Ciglitazone 抑制 th17 细胞的增殖和分化。Ciglitazone 是一种口服降糖剂，在肥胖高血糖动物模型中具有活性。Ciglitazone 诱导负鼠肾上皮细胞凋亡 (apoptosis)，同时激活 p38 MAPK 和凋亡诱导因子 (AIF) 的核转位。

Ciglitazone(Synonyms: 环格列酮; ADD-3878; U-63287)

Ciglitazone Chemical Structure

CAS No. : 74772-77-3

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生物活性

Ciglitazone is a potent and selective PPARγ agonist (EC50=3 μM). Ciglitazone inhibits proliferation and differentiation of th17 cells. Ciglitazone is a hypoglycemic agent orally active in the obese-hyperglycemic animal models. Ciglitazone induces apoptosis accompanied by activation of p38 MAPK and nuclear translocation of apoptosis inducing factor (AIF) in opossum kidney (OK) renal epithelial cells[1][2][3][4].

体外研究
(In Vitro)

Ciglitazone (0-20 μM; 24 hours) induces apoptosis through PPAR-independent mechanism. Ciglitazone causes generation of ROS and an increase in intracellular Ca2+[4].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

In C57BL/6J-ob/ob mice, Ciglitazone (100 mg/kg/day; 2 days) elicits a drastic fall in blood glucose. Regranulation of islet beta-cells and increased pancreatic insulin content are observed in ob/ob mice treated for 41-44 days with 100 mg/kg/day Ciglitazone[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

333.45

Formula

C18H23NO3S
CAS 号

74772-77-3
中文名称

环格列酮；酪里达唑
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
In solvent -80°C 6 months
-20°C 1 month
参考文献

  • [1]. Willson TM, et al. The structure-activity relationship between peroxisome proliferator-activated receptor gamma agonism and the antihyperglycemic activity of thiazolidinediones. J Med Chem. 1996;39(3):665-668.

    [2]. Kim DH, et al. Ciglitazone, a peroxisome proliferator-activated receptor gamma ligand, inhibits proliferation and differentiation of th17 cells. Biomol Ther (Seoul). 2015;23(1):71-76.

    [3]. Chang AY, et al. Ciglitazone, a new hypoglycemic agent. I. Studies in ob/ob and db/db mice, diabetic Chinese hamsters, and normal and streptozotocin-diabetic rats. Diabetes. 1983;32(9):830-838.

    [4]. Kwon CH, et al. Ciglitazone induces apoptosis via activation of p38 MAPK and AIF nuclear translocation mediated by reactive oxygen species and Ca(2+) in opossum kidney cells. Toxicology. 2009;257(1-2):1-9.

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