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.
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
Compound Libraries
BMS 182874 hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| 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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solubility | Soluble to 100 mM in DMSO |
Preparing Stock Solutions
The following data is based on the product molecular weight 381.88. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.62 mL | 13.09 mL | 26.19 mL |
| 5 mM | 0.52 mL | 2.62 mL | 5.24 mL |
| 10 mM | 0.26 mL | 1.31 mL | 2.62 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.52 mL |
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References
References are publications that support the products' biological activity.
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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