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Palosuran Sale

(Synonyms: ACT-058362) 目录号 : GC17414

A urotensin II receptor antagonist

Palosuran Chemical Structure

Cas No.:540769-28-6

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥2,302.00
现货
5mg
¥2,093.00
现货
10mg
¥3,199.00
现货
50mg
¥8,955.00
现货
100mg
¥15,300.00
现货

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Sample solution is provided at 25 µL, 10mM.

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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.

Chemical Properties

Cas No. 540769-28-6 SDF
别名 ACT-058362
化学名 1-[2-(4-benzyl-4-hydroxypiperidin-1-yl)ethyl]-3-(2-methylquinolin-4-yl)urea
Canonical SMILES CC1=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
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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1 mg 5 mg 10 mg
1 mM 2.3893 mL 11.9466 mL 23.8931 mL
5 mM 0.4779 mL 2.3893 mL 4.7786 mL
10 mM 0.2389 mL 1.1947 mL 2.3893 mL
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