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Submit ReviewBMS 182874 hydrochloride
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)
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 |
| InChI Key | UZZFRNZGYDOBAO-UHFFFAOYSA-N |
| 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
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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2 Citations for BMS 182874 hydrochloride
Citations are publications that use Tocris products. Selected citations for BMS 182874 hydrochloride include:
Yuan et al (2015) Endothelial cells enhance the migration of bovine meniscus cells. Arthritis Rheumatol 67 182 PMID: 25307081
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
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