Molecular structure of BMS 182874 hydrochloride, CAS Number: 1215703-04-0
BMS 182874 hydrochloride (CAS 1215703-04-0)
Application:
BMS 182874 hydrochloride is a competive non-peptide endothelin ETAR antagonist
CAS Number:
1215703-04-0
Molecular Weight:
381.88
Molecular Formula:
C17H19N3O3S•HCl
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
BMS 182874 hydrochloride is a potent, selective, and competitive non-peptide endothelin ETAR antagonist (Ki = 48 nM). It Displays > 1000-fold selectivity over ETB receptors. BMS 182874 hydrochloride inhibits ET-1-induced pressor response in vivo. It inhibits ET-1-induced pressor response, and also inhibits ET-1-induced longitudinal muscle contraction in vitro.
BMS 182874 hydrochloride (CAS 1215703-04-0) References
- ET(A) receptor antagonist prevents blood pressure elevation and vascular remodeling in aldosterone-infused rats. | Park, JB. and Schiffrin, EL. 2001. Hypertension. 37: 1444-9. PMID: 11408393
- Elevated mean arterial pressure in the ovariectomized rat was normalized by ET(A) receptor antagonist therapy: absence of cardiac hypertrophy and fibrosis. | Mercier, I., et al. 2002. Br J Pharmacol. 136: 685-92. PMID: 12086977
- Contribution of endothelin-1 to renal activator protein-1 activation and macrophage infiltration in aldosterone-induced hypertension. | Tostes, RC., et al. 2002. Clin Sci (Lond). 103 Suppl 48: 25S-30S. PMID: 12193048
- Cardiac fibrosis occurs early and involves endothelin and AT-1 receptors in hypertension due to endogenous angiotensin II. | Seccia, TM., et al. 2003. J Am Coll Cardiol. 41: 666-73. PMID: 12598081
- ETA receptor blockade decreases vascular superoxide generation in DOCA-salt hypertension. | Callera, GE., et al. 2003. Hypertension. 42: 811-7. PMID: 12913063
- Selective blockade of the endothelin subtype A receptor decreases early atherosclerosis in hamsters fed cholesterol. | Kowala, MC., et al. 1995. Am J Pathol. 146: 819-26. PMID: 7717449
- Antihypertensive effects of a novel endothelin-A receptor antagonist in rats. | Bird, JE., et al. 1995. Hypertension. 25: 1191-5. PMID: 7768562
- BMS-182874 is a selective, nonpeptide endothelin ETA receptor antagonist. | Webb, ML., et al. 1995. J Pharmacol Exp Ther. 272: 1124-34. PMID: 7891325
- EndothelinB receptor-mediated contraction of human and rat pulmonary resistance arteries and the effect of pulmonary hypertension on endothelin responses in the rat. | McCulloch, KM. and MacLean, MR. 1995. J Cardiovasc Pharmacol. 26 Suppl 3: S169-76. PMID: 8587353
- Orally active endothelin receptor antagonist BMS-182874 suppresses neointimal development in balloon-injured rat carotid arteries. | Ferrer, P., et al. 1995. J Cardiovasc Pharmacol. 26: 908-15. PMID: 8606527
- Mutational analysis of the endothelin type A receptor (ETA): interactions and model of selective ETA antagonist BMS-182874 with putative ETA receptor binding cavity. | Webb, ML., et al. 1996. Biochemistry. 35: 2548-56. PMID: 8611558
- Influence of specific and non-specific endothelin receptor antagonists on renal morphology in rats with surgical renal ablation. | Nabokov, A., et al. 1996. Nephrol Dial Transplant. 11: 514-20. PMID: 8671823
- A role for endothelin ETA receptors in regulation of renal function in spontaneously hypertensive rats. | Bird, JE., et al. 1995. Eur J Pharmacol. 294: 183-9. PMID: 8788430
- Pharmacology of two novel mixed ETA/ETB receptor antagonists, BQ-928 and 238, in the carotid and pulmonary arteries and the perfused kidney of the rabbit. | Maurice, MC., et al. 1997. Br J Pharmacol. 120: 319-25. PMID: 9117126
- The ETA receptor antagonist, BMS-182874, reduces acute hypoxic pulmonary hypertension in pigs in vivo. | Holm, P., et al. 1998. Cardiovasc Res. 37: 765-71. PMID: 9659461
Inhibitor of:
ETAR.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
BMS 182874 hydrochloride, 5 mg | sc-361123 | 5 mg | $185.00 | |||
BMS 182874 hydrochloride, 25 mg | sc-361123A | 25 mg | $580.00 |