(S)-2-甲氧基-3-[4-[2-(5-甲基-2-苯基恶唑-4-基)乙氧基]苯并[B]噻吩-7-基]丙酸

• 常用名: (S)-2-甲氧基-3-[4-[2-(5-甲基-2-苯基恶唑-4-基)乙氧基]苯并[B]噻吩-7-基]丙酸
• 英文名: Aleglitazar
• CAS号: 475479-34-6
• 分子量: 437.50800
• 密度: 1.29
• 沸点: 665.151ºC at 760 mmHg
• 分子式: C₂₄H₂₃NO₅S
• 熔点: N/A
• 闪点: 356.071ºC

用途

Aleglitazar(R1439; RO-0728804)是PPAR-α/γ激动剂,IC50分别为2.8 nM/4.6 nM。

名称

• 中文名: 阿格列扎
• 英文名: (2S)-2-methoxy-3-[4-[2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethoxy]-1-benzothiophen-7-yl]propanoic acid
• 中文别名: (S)-2-甲氧基-3-[4-[2-(5-甲基-2-苯基恶唑-4-基)乙氧基]苯并[B]噻吩-7-基]丙酸

生物活性

• 描述: Aleglitazar(R1439; RO-0728804)是PPAR-α/γ激动剂,IC50分别为2.8 nM/4.6 nM。
• 相关类别:
  研究领域 >> 代谢疾病
• 靶点:

  PPARγ:19 nM (IC50)

  PPARα:38 nM (IC50)

• 参考文献:

  [1]. Bénardeau A, Verry P, Atzpodien EA, et al. Effects of the dual PPAR-α/γ agonist aleglitazar on glycaemic control and organ protection in the Zucker diabetic fatty rat. Diabetes Obes Metab. 2013 Feb;15(2):164-74.

  [2]. Younk LM, Uhl L, Davis SN. Pharmacokinetics, efficacy and safety of aleglitazar for the treatment of type 2 diabetes with high cardiovascular risk. Expert Opin Drug Metab Toxicol. 2011 Jun;7(6):753-63.

  [3]. Foley-Comer AJ, Young AM, Russell-Yarde F, et al. Aleglitazar, a balanced PPARα/γ agonist, has no clinically relevant pharmacokinetic interaction with high-dose atorvastatin or rosuvastatin. Expert Opin Investig Drugs. 2011 Jan;20(1):3-12.

  [4]. Cavender MA, Lincoff AM. Therapeutic potential of aleglitazar, a new dual PPAR-α/γ agonist: implications for cardiovascular disease in patients with diabetes mellitus. Am J Cardiovasc Drugs. 2010;10(4):209-16.

  [5]. Bénardeau A, Benz J, Binggeli A, et al. Aleglitazar, a new, potent, and balanced dual PPARalpha/gamma agonist for the treatment of type II diabetes. Bioorg Med Chem Lett. 2009 May 1;19(9):2468-73.

物理化学性质

• 密度: 1.29
• 沸点: 665.151ºC at 760 mmHg
• 分子式: C₂₄H₂₃NO₅S
• 分子量: 437.50800
• 闪点: 356.071ºC
• 精确质量: 437.13000
• PSA: 110.03000
• LogP: 5.12830
• 折射率: 1.627
• 储存条件: 2-8℃

英文别名

• UNII-41T4OAG59U
• R-1439
• Aleglitazar