BMS 182874 hydrochloride
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.
Sold with the permission of Bristol-Myers Squibb Company, subject to U.S. Patent No. 5,378,715 and other US and foreign patents
|Storage||Store at RT|
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||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|
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
If you know of a relevant reference for BMS 182874 hydrochloride, please let us know.
View Related Products by Product Action
Keywords: BMS 182874 hydrochloride, supplier, selective, orally, active, non-peptide, ETA, antagonists, receptors, endothelin, BMS182874, hydrochloride, Endothelin, ETA, Receptors, Endothelin, ETA, Receptors, 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
Do you know of a great paper that uses BMS 182874 hydrochloride from Tocris? If so please let us know.
BMS 182874 hydrochloride Reviews
Average Rating:(Based on 0 Reviews)
Literature in this Area
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.