SB 706375

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Cat.No. 4667 - SB 706375 | C20H22BrF3N2O5S | CAS No. 733734-61-7
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)
Datasheet
Citations
Literature

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.

Select a batch to recalculate based on the batch molecular weight:
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

Safety Datasheet

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


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

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