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
Compound Libraries
SB 657510 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| 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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 50.58 | 100 |
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 solvent 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 |
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Product Datasheets
References
References are publications that support the products' biological activity.
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
Keywords: SB 657510, supplier, SB657510, UT-II, urotensin-II, receptors, antagonists, GlaxoSmithKline, Urotensin-II, Receptors, Urotensin-II, Receptors, Tocris Bioscience
