SB 657510
Discontinued Product
Chemical Name: 2-Bromo-N-[4-chloro-3-[[(3R)-1-methyl-3-pyrrolidinyl]oxy]phenyl]-4,5-dimethoxybenzenesulfonamide
Purity: ≥98%
Biological Activity
SB 657510 is a selective urotensin-II (UT) receptor antagonist (Ki values are 61, 17, 30, 65 and 56 nM at human, monkey, cat, rat and mouse receptors respectively). Inhibits U-II-induced intracellular Ca2+ mobilization (IC50 = 180 nM) and antagonizes the contractile action of U-II in isolated mammalian arteries and aortae (EC50 = 50 - 189 nM).Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Additional Information
Background References
-
Nonpeptide urotensin-II receptor antagonists I: in vitro pharmacological characterization of SB-706375.
Douglas et al.
Br.J.Pharmacol., 2005;145:620 -
Palosuran inhibits binding to primate UT receptors in cell membranes but demonstrates differential activity in intact cells and vascular tissues.
Behm et al.
Br.J.Pharmacol., 2008;155:374
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