Catalog Number: 1441
Chemical Name: 5-(Dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulfonamide hydrochloride
Biological Activity
Potent, selective and competitive non-peptide endothelin ETA receptor antagonist (Ki = 48 nM). Displays > 1000-fold selectivity over ETB receptors. Inhibits ET-1-induced pressor response following oral or intravenous administration in vivo. Inhibits ET-1-induced longitudinal muscle contraction in the mouse colon in vitro.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
  • Storage:
    Store at RT
  • CAS No:
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.
Additional Information
Licensing Caveats:
Sold with the permission of Bristol-Myers Squibb Company, subject to U.S. Patent No. 5,378,715 and other US and foreign patents
Background References
  1. Pharmacological characterization of endothelin receptors-mediated contraction in the mouse isolated proximal and distal colon.
    Khan et al.
    Br.J.Pharmacol., 2006;147:607
  2. BMS-182874 is a selective, nonpeptide endothelin ETA receptor antagonist.
    Webb et al.
    J.Pharmacol.Exp.Ther., 1995;272:1124
  3. The discovery of sulfonamide endothelin antagonists and the development of the orally active ETA antagonist 5-(Dimethylamino)-N-(3,4-dimethyl-5-isoazolyl)-1-naphthalenesulfonamide.
    Stein et al.
    J.Med.Chem., 1994;37:329

The citations listed below are publications that use Tocris products. Selected citations for BMS 182874 hydrochloride include:

Showing Results 1 - 2 of 2

  1. Endothelial cells enhance the migration of bovine meniscus cells.
    Authors: Yuan Et al.
    Arthritis Rheumatol
  2. Pharmacological characterization of endothelin receptors-mediated contraction in the mouse isolated proximal and distal colon.
    Authors: Khan Et al.
    Br J Pharmacol
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