SB 706375

Cat. No. 4667

SB 706375 C20H22BrF3N2O5S [733734-61-7]

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Chemical Name: 2-Bromo-4,5-dimethoxy-N-[3-[[(3R)-1-methyl-3-pyrrolidinyl]oxy]-4-(trifluoromethyl)phenyl]benzenesulfonamide

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.

Technical Data

M.Wt:
539.36
Formula:
C20H22BrF3N2O5S
Solubility:
Soluble to 100 mM in DMSO
Purity:
>98 %
Storage:
Store at RT
CAS No:
733734-61-7

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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

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.

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Keywords: SB 706375, supplier, SB706375, urotensin-II, U-II, receptors, UT, antagonists, high, affinity, Tocris Bioscience, Urotensin-II Receptor Antagonist products

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