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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).
Sold with the permission of GlaxoSmithKline
|Storage||Store at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 505.81. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.98 mL||9.89 mL||19.77 mL|
|5 mM||0.4 mL||1.98 mL||3.95 mL|
|10 mM||0.2 mL||0.99 mL||1.98 mL|
|50 mM||0.04 mL||0.2 mL||0.4 mL|
References are publications that support the biological activity of the product.
Douglas et al (2005) Nonpeptide urotensin-II receptor antagonists I: in vitro pharmacological characterization of SB-706375. Br.J.Pharmacol. 145 620 PMID: 15852036
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
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Keywords: SB 657510, SB 657510 supplier, SB657510, UT-II, urotensin-II, receptors, antagonists, GlaxoSmithKline, Urotensin-II, Receptors, 3571, Tocris Bioscience
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