Toggle Nav
Close
  • Menu
  • Setting

Palosuran

Catalog No.
B1304
Urotensin-II receptor antagonist
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$294.00
In stock
5mg
$230.00
In stock
10mg
$350.00
In stock
25mg
$586.00
In stock
50mg
$795.00
In stock
100mg
$1,235.00
Ship with 10-15 days

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

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

Physical AppearanceA solid
StorageStore at -20°C
M.Wt418.53
Cas No.540769-28-6
FormulaC25H30N4O2
Solubility≥2.25 mg/mL in EtOH with gentle warming and ultrasonic; ≥2.33 mg/mL in H2O with gentle warming and ultrasonic; ≥8.95 mg/mL in DMSO with gentle warming
Chemical Name1-[2-(4-benzyl-4-hydroxypiperidin-1-yl)ethyl]-3-(2-methylquinolin-4-yl)urea
SDFDownload SDF
Canonical SMILESCC1=NC2=CC=CC=C2C(=C1)NC(=O)NCCN3CCC(CC3)(CC4=CC=CC=C4)O
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Quality Control