540769-28-6

• 常用中文名：ACT 058362; PALOSURAN,
• 常用英文名：Palosuran
• CAS号：540769-28-6
• 分子式：C₂₅H₃₀N₄O₂
• 分子量：418.53100
• 相关类别： 信号通路 G 蛋白偶联受体/G 蛋白 Urotensin Receptor
• 发布时间：2016-04-18 11:08:40
• 更新时间：2024-01-07 16:51:26
• Palosuran (ACT-058362)是高活性人UT受体特异性拮抗剂，IC50为3.6 nM。

名称

• 中文名: Palosuran
• 英文名: 1-[2-(4-benzyl-4-hydroxypiperidin-1-yl)ethyl]-3-(2-methylquinolin-4-yl)urea
• 英文别名: UNII-ULD9ZKE457; Palosuran; ACT 058362; Urea, N-[2-[4-hydroxy-4-(phenylMethyl)-1-piperidinyl]ethyl]-N'-(2-Methyl-4-quinolinyl)-

物化性质

• 分子式: C₂₅H₃₀N₄O₂
• 分子量: 418.53100
• 精确质量: 418.23700
• PSA: 84.21000
• LogP: 3.29850
• 外观性状: white solid
• 储存条件: -20℃

生物活性

• 描述: Palosuran (ACT-058362)是高活性人UT受体特异性拮抗剂,IC50为3.6 nM。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> Urotensin Receptor
  研究领域 >> 代谢疾病
• 参考文献:

  [1]. Clozel M, et al. Pharmacology of the urotensin-II receptor antagonist palosuran (ACT-058362; 1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-urea sulfate salt): first demonstration of a pathophysiological role of the urotensin S

  [2]. Clozel M, et al. The urotensin-II receptor antagonist palosuran improves pancreatic and renal function in diabetic rats. J Pharmacol Exp Ther. 2006 Mar;316(3):1115-21.

  [3]. Sidharta PN, et al. Pharmacodynamics and pharmacokinetics of the urotensin II receptor antagonist palosuran in macroalbuminuric, diabetic patients. Clin Pharmacol Ther. 2006 Sep;80(3):246-56.

  [4]. Trebicka J, et al. Hemodynamic effects of urotensin II and its specific receptor antagonist palosuran in cirrhotic rats. Hepatology. 2008 Apr;47(4):1264-76.

  [5]. Sidharta PN, et al. Pharmacokinetics and pharmacodynamics of the urotensin-II receptor antagonist palosuran in healthy male subjects. J Clin Pharmacol. 2009 Oct;49(10):1168-75.