BMS 182874 hydrochloride

Discontinued Product

BMS 182874 hydrochloride (Cat. No. 1441) has been withdrawn from sale for commercial reasons.
Description: Highly selective, orally active non-peptide ETA antagonist
Chemical Name: 5-(Dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulfonamide hydrochloride
Purity: ≥98% (HPLC)
Citations (2)
Literature (5)

Biological Activity for BMS 182874 hydrochloride

BMS 182874 hydrochloride is a 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.

Licensing Information

Sold with the permission of Bristol-Myers Squibb Company, subject to U.S. Patent No. 5,378,715 and other US and foreign patents

Technical Data for BMS 182874 hydrochloride

M. Wt 381.88
Formula C17H19N3O3S.HCl
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 1215703-04-0
PubChem ID 56972163
Smiles Cl.CN(C)C1=C2C=CC=C(C2=CC=C1)S(=O)(=O)NC1=C(C)C(C)=NO1

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.

Product Datasheets for BMS 182874 hydrochloride

Certificate of Analysis / Product Datasheet
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References for BMS 182874 hydrochloride

References are publications that support the biological activity of the product.

Khan et al (2006) Pharmacological characterization of endothelin receptors-mediated contraction in the mouse isolated proximal and distal colon. Br.J.Pharmacol. 147 607 PMID: 16432510

Stein et al (1994) 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. J.Med.Chem. 37 329 PMID: 8308857

Webb et al (1995) BMS-182874 is a selective, nonpeptide endothelin ETA receptor antagonist. J.Pharmacol.Exp.Ther. 272 1124 PMID: 7891325

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Keywords: BMS 182874 hydrochloride, BMS 182874 hydrochloride supplier, selective, orally, active, non-peptide, ETA, antagonists, receptors, endothelin, BMS182874, hydrochloride, Endothelin, Receptors, 1441, Tocris Bioscience

2 Citations for BMS 182874 hydrochloride

Citations are publications that use Tocris products. Selected citations for BMS 182874 hydrochloride include:

Khan et al (2006) Pharmacological characterization of endothelin receptors-mediated contraction in the mouse isolated proximal and distal colon. Br J Pharmacol 147 607 PMID: 16432510

Yuan et al (2015) Endothelial cells enhance the migration of bovine meniscus cells. Arthritis Rheumatol 67 182 PMID: 25307081

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Literature in this Area

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