Palosuran (hydrochloride)

Palosuran hydrochloride (ACT-058362 hydrochloride) is a potent, selective, and orally active antagonist of urotensin II receptor, with an IC50 of 3.6 nM for CHO cell membranes expressing human recombinant receptors. Palosuran hydrochloride can improves pancreatic and renal function in diabetic rats[1][2].

Product Specifications

CAS Number

[2469274-58-4]

Product Name Alternative

ACT-058362 (hydrochloride)

UNSPSC

12352005

Target

Urotensin Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

Neuroscience-Neuromodulation

Field of Research

Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/palosuran-hydrochloride.html

Purity

98.67

Solubility

DMSO : 50 mg/mL (ultrasonic) |H2O : 7.14 mg/mL (ultrasonic)

Smiles

OC(CC1=CC=CC=C1)(CC2)CCN2CCNC(NC3=CC(C)=NC4=CC=CC=C34)=O.[H]Cl

Molecular Formula

C25H31ClN4O2

Molecular Weight

454.99

References & Citations

[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 System. J Pharmacol Exp Ther. 2004 Oct;311 (1) :204-12.|[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.