Edaglitazone

• 常用名: Edaglitazone
• 英文名: Edaglitazone
• CAS号: 213411-83-7
• 分子量: 464.56
• 密度: 1.4±0.1 g/cm3
• 沸点: N/A
• 分子式: C₂₄H₂₀N₂O₄S₂
• 熔点: N/A
• 闪点: N/A

Edaglitazone用途

依达格列酮是一种有效、选择性和口服活性的PPARγ激动剂,PPARα和PPARγ的EC50分别为35.6nm和1053nm。依达格列酮具有抗血小板、降糖和降血糖活性[1][2][3]。

Edaglitazone名称

• 英文名: 5-[[4-[2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethoxy]-1-benzothiophen-7-yl]methyl]-1,3-thiazolidine-2,4-dione

Edaglitazone生物活性

• 描述: 依达格列酮是一种有效、选择性和口服活性的PPARγ激动剂,PPARα和PPARγ的EC50分别为35.6nm和1053nm。依达格列酮具有抗血小板、降糖和降血糖活性[1][2][3]。
• 相关类别:
  信号通路 >> 细胞周期/DNA损伤 >> PPAR
• 靶点:

  PPARγ:35.6 nM (EC50)

  PPARα:1053 nM (EC50)

• 体外研究: 依达格列酮(3-16μM；5min)抑制胶原(1.2μg/mL)诱导的血小板聚集。依达格列酮以浓度依赖性方式增加血小板内cAMP水平。依达格列酮可预防胶原诱导的血小板内PPARγ水平降低[3]。
• 体内研究: 依达格列酮(4.4 mg/kg；连续10天每天一次)提高肥胖大鼠的胰岛素敏感性[2]。
• 参考文献:

  [1]. Dietz M, et, al. Comparative molecular profiling of the PPARα/γ activator aleglitazar: PPAR selectivity, activity and interaction with cofactors. ChemMedChem. 2012 Jun;7(6):1101-11.

  [2]. Fürnsinn C, et, al. Chronic and acute effects of thiazolidinediones BM13.1258 and BM15.2054 on rat skeletal muscle glucose metabolism. Br J Pharmacol. 1999 Nov;128(6):1141-8.

  [3]. Muñoz-Gutiérrez C, et, al. Study of the interactions between Edaglitazone and Ciglitazone with PPARγ and their antiplatelet profile. Life Sci. 2017 Oct 1;186:59-65.

Edaglitazone物理化学性质

• 密度: 1.4±0.1 g/cm3
• 分子式: C₂₄H₂₀N₂O₄S₂
• 分子量: 464.56
• 精确质量: 464.086456
• PSA: 138.46000
• LogP: 6.20
• 折射率: 1.673

Edaglitazone英文别名

• UNII:8GKF7V499B
• EX-8519
• 5-({4-[2-(5-Methyl-2-phenyl-1,3-oxazol-4-yl)ethoxy]-1-benzothiophen-7-yl}methyl)-1,3-thiazolidine-2,4-dione
• UNII-8GKF7V499B
• Edaglitazone
• 2,4-Thiazolidinedione, 5-[[4-[2-(5-methyl-2-phenyl-4-oxazolyl)ethoxy]benzo[b]thien-7-yl]methyl]-
• 5-((4-(2-(5-methyl-2-phenyloxazol-4-yl)ethoxy)benzo[b]thiophen-7-yl)methyl)thiazolidine-2,4-dione