Description: High affinity, non-peptide UT receptor antagonist
Chemical Name: 2-Bromo-4,5-dimethoxy-N-[3-[[(3R)-1-methyl-3-pyrrolidinyl]oxy]-4-(trifluoromethyl)phenyl]benzenesulfonamide
Purity: ≥98% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
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.
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
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Douglaset al (2005) Nonpeptidic urotensin-II receptor antagonists I: in vitro pharmacological characterization of SB-706375. Br.J.Pharmacol. 145 620 PMID: 15852036