Chemical Structure : SB-706375
CAS No.:
733734-61-7
SB-706375
(SB706375)
Catalog No.: PC-28274Not For Human Use, Lab Use Only.
SB-706375 is a potent, selective nonpeptidic urotensin-II receptor (U-II) antagonist, potently inhibits [(125)I]hU-II binding to both mammalian recombinant UT receptors (Ki=4.7-20.7 nM at rodent, feline and primate recombinant UT receptors) and Ki 5.4 nM at the endogenous UT receptor in SJRH30 cells.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
SB-706375 is a potent, selective nonpeptidic urotensin-II receptor (U-II) antagonist, potently inhibits [(125)I]hU-II binding to both mammalian recombinant UT receptors (Ki=4.7-20.7 nM at rodent, feline and primate recombinant UT receptors) and Ki 5.4 nM at the endogenous UT receptor in SJRH30 cells.
SB-706375 is a potent, competitive hU-II antagonist across species with pK(b) 7.29-8.00 in HEK293-UT receptor cells (inhibition of [Ca(2+)](i)-mobilization) and pK(b) 7.47 in rat isolated aorta (inhibition of contraction).
SB-706375 also reversed tone established in the rat aorta by prior exposure to hU-II (K(app) approximately 20 nM).
Physicochemical Properties
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M.Wt
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539.36
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Formula
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C20H22BrF3N2O5S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(R)-2-Bromo-4,5-dimethoxy-N-(3-((1-methylpyrrolidin-3-yl)oxy)-4-(trifluoromethyl)phenyl)benzenesulfonamide
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References
1. Douglas SA, et al. Br J Pharmacol. 2005 Jul;145(5):620-35.
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