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Palosuran
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。
Palosuran图片
CAS NO:540769-28-6
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
Palosuran (ACT-058362) 是一种有效的、选择性的、口服活性的 urotensin II 受体拮抗剂，对表达人重组受体的 CHO 细胞膜的 IC50 为 3.6 nM。
Cas No.540769-28-6
别名ACT-058362
化学名1-[2-(4-benzyl-4-hydroxypiperidin-1-yl)ethyl]-3-(2-methylquinolin-4-yl)urea
Canonical SMILESCC1=NC2=CC=CC=C2C(=C1)NC(=O)NCCN3CCC(CC3)(CC4=CC=CC=C4)O
分子式C25H30N4O2
分子量418.53
溶解度≥ 8.95mg/mL in DMSO with gentle warming
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Palosuran is a potent and specific antagonist of human urotensin-II receptor with IC50 value of 3.6nM [1].

Palosuran is a nonpeptidic, potent and selective antagonist of the urotensin-II receptor. It is selective toward human receptor. The IC50 value of it to rat receptor is 1475nM. The efficacy of palosuran to inhibit Ca2+ mobilization in CHO cells also improved that palosuran is more effective to human UT receptors than to rat UT receptors with IC50 values of 17nM and more than 10μM, respectively. Besides that, palosuran inhibits the phosphorylation of MAPK with IC50 value of 150nM in recombinant CHO cells. Palosuran is selective. It shows no inhibition of other receptors involved in vascular tone regulation such as α-1 adrenoceptor, 5-hydroxytryptamine 2A receptor and endothelin receptor A. Palosuran is used as a pharmacological tool to study the role of endogenous U-II [1, 2].

References:
[1] Carotenuto A, Grieco P, Rovero P, et al. Urotensin-II receptor antagonists. Current medicinal chemistry, 2006, 13(3): 267-275.
[2] Clozel M, Binkert C, Birker-Robaczewska 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 system. Journal of Pharmacology and Experimental Therapeutics, 2004, 311(1): 204-212.