SB 657510

Cat. No. 3571

SB 657510 C19H22BrClN2O5S [474960-44-6]

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Chemical Name: 2-Bromo-N-[4-chloro-3-[[(3R)-1-methyl-3-pyrrolidinyl]oxy]phenyl]-4,5-dimethoxybenzenesulfonamide

Biological Activity

Selective urotensin-II (UT) receptor antagonist (Ki values are 61, 17, 30, 65 and 56 nM at human, monkey, cat, rat and mouse receptors respectively). Inhibits U-II-induced intracellular Ca2+ mobilization (IC50 = 180 nM) and antagonizes the contractile action of U-II in isolated mammalian arteries and aortae (EC50 = 50 - 189 nM).

Licensing Information

Sold with the permission of GlaxoSmithKline

Technical Data

M.Wt:
505.81
Formula:
C19H22BrClN2O5S
Solubility:
Soluble to 100 mM in DMSO
Purity:
>98 %
Storage:
Store at RT
CAS No:
474960-44-6

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Behm et al (2008) Palosuran inhibits binding to primate UT receptors in cell membranes but demonstrates differential activity in intact cells and vascular tissues. Br.J.Pharmacol. 155 374. PMID: 18587423.

Douglas et al (2005) Nonpeptide urotensin-II receptor antagonists I: in vitro pharmacological characterization of SB-706375. Br.J.Pharmacol. 145 620. PMID: 15852036.

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Keywords: SB 657510, supplier, SB657510, UT-II, urotensin-II, receptors, antagonists, GlaxoSmithKline, Tocris Bioscience, Urotensin-II Receptor Antagonist products

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