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Submit ReviewSB 657510
Description: Selective urotensin-II (UT) receptor antagonist
Chemical Name: 2-Bromo-N-[4-chloro-3-[[(3R)-1-methyl-3-pyrrolidinyl]oxy]phenyl]-4,5-dimethoxybenzenesulfonamide
Purity: ≥98% (HPLC)
Biological Activity for SB 657510
SB 657510 is a 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 for SB 657510
| M. Wt | 505.81 |
| Formula | C19H22BrClN2O5S |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 474960-44-6 |
| PubChem ID | 11272107 |
| InChI Key | KQCZCINJGIRLCD-CYBMUJFWSA-N |
| Smiles | BrC1=CC(OC)=C(OC)C=C1S(NC2=CC=C(Cl)C(O[C@H]3CN(C)CC3)=C2)(=O)=O |
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.
Product Datasheets for SB 657510
References for SB 657510
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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