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Palosuran hydrochloride 540769-28-6(free base）

Catalog No. T4689 CAS T4689

Synonyms: ACT-058362 hydrochloride

Palosuran hydrochloride 540769-28-6(free base)(ACT-058362 hydrochloride) is a new potent and specific antagonist of the human UT receptor with an IC50 of 3.6±0.2 nM.

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Palosuran hydrochloride 540769-28-6(free base） Chemical Structure

Palosuran hydrochloride 540769-28-6(free base）, CAS T4689

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Biological Description

Chemical Properties

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Description	Palosuran hydrochloride 540769-28-6(free base)(ACT-058362 hydrochloride) is a new potent and specific antagonist of the human UT receptor with an IC50 of 3.6±0.2 nM.
Targets&IC50	GPR14:3.6 nM
In vitro	Palosuran inhibited 125I-U-II binding to human UT receptors in membrane preparations from CHO cells carrying the human UT receptors almost as potently as cold U-II, with an IC50 of 3.6 ± 0.2 nM. On cells, the inhibitory binding potency of palosuran against human UT receptor was lower than on membranes (IC50 = 46.2 ± 13 nM on TE 671 cells and 86 ± 30 nM on recombinant CHO cells). Compared with the human UT receptor, the binding inhibitory potency of palosuran against the rat UT receptor was lower in membrane preparation (400-fold), as well as in cells (>120-fold) [1].
In vivo	Long-term treatment of streptozotocin-induced diabetic rats with palosuran improved survival, increased insulin, and slowed the increase in glycemia, glycosylated hemoglobin, and serum lipids. Furthermore, palosuran increased renal blood flow and delayed the development of proteinuria and renal damage [2]. Palosuran was rapidly absorbed with maximum plasma concentrations at 1 hour after drug administration. The accumulation factor was 1.7 (geometric mean) (95% confidence interval, 1.3 to 2.1).Palosuran was well tolerated [3]. In mesenteric vessels, palosuran treatment up-regulated expression of RhoA and Rho-kinase, increased Rho-kinase-activity, and diminished nitric oxide (NO)/cyclic guanosine 3',5'-monophosphate (cGMP) signaling. Moreover, palosuran increased renal blood flow, sodium, and water excretion in BDL rats [4].

Synonyms	ACT-058362 hydrochloride
Molecular Weight	454.99
Formula	C25H31ClN4O2
CAS No.	T4689

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: >30 mg/mL

References and Literature

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]. J Pharmacol Exp Ther, 2004, 311(1):204-212. 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.

Related compound libraries

This product is contained In the following compound libraries：

Endocrinology-Hormone Compound Library NO PAINS Compound Library

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Keywords

Palosuran hydrochloride 540769-28-6(free base） T4689 Endocrinology/Hormones GPCR/G Protein GPR Palosuran hydrochloride 540769-28-6(free base) ACT058362 Hydrochloride ACT-058362 Hydrochloride Palosuran hydrochloride 540769286(free base） ACT-058362 hydrochloride Palosuran hydrochloride 540769 28 6(free base） ACT 058362 Hydrochloride inhibitor inhibit

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