Palosuran (Synonyms: ACT058362) |
| Katalog-Nr.GC17414 |
Palosuran (ACT-058362) ist ein potenter, selektiver und oral aktiver Antagonist des Urotensin-II-Rezeptors mit einem IC50-Wert von 3,6 nM fÜr CHO-Zellmembranen, die humane rekombinante Rezeptoren exprimieren.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 540769-28-6
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 540769-28-6 | SDF | |
| Überlieferungen | ACT058362 | ||
| Chemical Name | 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 | ||
| Formula | C25H30N4O2 | M.Wt | 418.53 |
| Löslichkeit | ≥ 8.95mg/mL in DMSO with gentle warming | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >99.00%
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Average Rating: 5 (Based on Reviews and 25 reference(s) in Google Scholar.)
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