Cat. No. Name Size Price Add Cart
KI2531SB70637510 mg$439.4
SB70637550 mg$2051.4

Chemical Characteristic

Product NameSB706375
SynonymsN/A
CAS No.733734-61-7
Molecular Weight 539.36
FormulaC20H22BrF3N2O5S
Chemical Name2-Bromo-4,5-dimethoxy-N-[3-[[(3R)-1-methyl-3-pyrrolidinyl]oxy]-4-(trifluoromethyl)phenyl]benzenesulfonamide
Smilesc1(c(cc(c(c1)OC)OC)Br)S(=O)(=O)Nc1cc(c(cc1)C(F)(F)F)OC1CN(CC1)C
Chemical Structure

Biological activities

SB706375 is a potent, reversible and selective mammalian UT receptor antagonist. SB706375 inhibits [125I] human urotensin II (hUII) binding to the UT receptor in SJRH30 cells, with a Ki of 5.4 nM. SB706375 also inhibits [125I] human urotensin II (hUII) binding to the rodent, feline, and primate recombinant UT receptors, with Ki values ranging from 4.7 to 20.7 nM.[1] SB706375 is a selective antagonist against both hUT2R and rUT2R, with Kd values of 9 and 21 nM, respectively.[2] SB706375 exhibits high-affinity cross-species antagonism, serving as a useful agent in delineating the pathophysiological actions of urotensin II in mammals.[1]

Protocols

In vitro, SB706375 is dissolved in DMSO.[1]

References

[1] Douglas SA, et al. Nonpeptidic urotensin-II receptor antagonists I: in vitro pharmacological characterization of SB-706375. Br J Pharmacol. 2005, 145(5): 620-635.
[2] Kim SK, et al. Prediction of the three-dimensional structure for the rat urotensin II receptor, and comparison of the antagonist binding sites and binding selectivity between human and rat receptors from atomistic simulations. ChemMedChem. 2010, 5(9): 1594-1608.

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