Chemical Name: 2-Bromo-N-[4-chloro-3-[[(3R)-1-methyl-3-pyrrolidinyl]oxy]phenyl]-4,5-dimethoxybenzenesulfonamide
Biological ActivitySelective 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).
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.
Nonpeptide urotensin-II receptor antagonists I: in vitro pharmacological characterization of SB-706375.
Douglas et al.
Palosuran inhibits binding to primate UT receptors in cell membranes but demonstrates differential activity in intact cells and vascular tissues.
Behm et al.
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