Biological Activity
High affinity, non-peptide antagonist of the urotensin-II (UT) receptor. Exhibits high affinity for mammalian UT receptors, including human, mouse and rat (Ki values are 9.3, 19.1 and 20.7 nM respectively, in HEK293 cells expressing recombinant UT receptors). Also inhibits binding of radiolabeled urotensin to endogenous human UT receptors (Ki = 5.4 nM in a whole-cell binding assay). Displays ≥100-fold selectivity for the human UT receptor over 86 different receptors, ion channels, enzymes, transporters and nuclear hormones.
Licensing Information
Sold for research purposes under agreement from GlaxoSmithKline.
Compound Libraries
SB 706375 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 539.36 |
| Formula | C20H22BrF3N2O5S |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 733734-61-7 |
| PubChem ID | 21023902 |
| InChI Key | BPOWQJYAMDEAFF-CYBMUJFWSA-N |
| Smiles | BrC1=CC(OC)=C(OC)C=C1S(NC2=CC=C(C(F)(F)F)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 | 53.94 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 539.36. 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 | 1.85 mL | 9.27 mL | 18.54 mL |
| 5 mM | 0.37 mL | 1.85 mL | 3.71 mL |
| 10 mM | 0.19 mL | 0.93 mL | 1.85 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.37 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Douglas et al (2005) Nonpeptidic urotensin-II receptor antagonists I: in vitro pharmacological characterization of SB-706375. Br.J.Pharmacol. 145 620 PMID: 15852036
Keywords: SB 706375, supplier, SB706375, urotensin-II, U-II, receptors, UT, antagonists, high, affinity, Urotensin-II, Receptors, Urotensin-II, Receptors, Tocris Bioscience
