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BMS 182874 hydrochloride
BMS 182874 hydrochloride is a nonpeptide endothelin (El) receptor antagonist.
Catalog No. T21790Cas No. 1215703-04-0
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Purity:97.01%
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BMS 182874 hydrochloride
Catalog No. T21790Cas No. 1215703-04-0
BMS 182874 hydrochloride is a nonpeptide endothelin (El) receptor antagonist.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose. | Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $74 | In Stock | |
| 2 mg | $98 | In Stock | |
| 5 mg | $151 | In Stock | |
| 10 mg | $227 | In Stock | |
| 25 mg | $381 | In Stock | |
| 50 mg | $531 | In Stock | |
| 100 mg | $738 | In Stock | |
| 200 mg | $996 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $157 | In Stock |
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Bosentan
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Bosentan (Benzenesulfonamide) is a sulfonamide-derived, competitive and specific endothelin receptor antagonist with a slightly higher affinity for the endothelin A receptor than endothelin B receptor. Bosentan blocks the action of endothelin 1, an extremely potent endogenous vasoconstrictor and bronchoconstrictor, by binding to endothelin A and endothelin B receptors in the endothelium and vascular smooth muscle. Bosentan decreases both pulmonary and systemic vascular resistance and is particularly used in the treatment of pulmonary arterial hypertension.
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BMS 182874 is an orally effective and highly selective endothelin receptor ETA antagonist with an IC50 value of 0.150 μM for ETA and a Ki value of 0.055 μM for ETA.BMS 182874 is able to reduce arterial pressure in a rat hypertension model induced by Deoxycorticosterone acetate. BMS 182874 was able to reduce Deoxycorticosterone-induced arterial pressure in a rat model of hypertension and can be used to study cardiovascular disease.
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Product Introduction
Bioactivity
Chemical Properties
| Description | BMS 182874 hydrochloride is a nonpeptide endothelin (El) receptor antagonist. |
| In vitro | BMS-l 82874 inhibited ET-l -stimulated inositol phosphate accumulation (KB 75 nM) and calcium mobilization (Ki = 140 nM) without suppressing the maximal responses in VSM-A10 cells. BMS-182874 competitively inhibited the binding of [125I]ET-1 to ETA receptors in rat vascular smooth muscle A10 (VSM-A10) cell membranes (Ki = 61 nM) and in CHO cells stably expressing the human ETA receptor (Ki = 48 nM), but was a weak inhibitor at ETB receptors (Ki > 50 μM) and non-ET receptors. |
| In vivo | BMS-182874 blunted the pressor response to exogenous ET-l when administered either orally (ED50 = 30 μmol/kg) or intravenously (ED50 = 24 μmol/kg) to conscious, normotensive rats. |
| Molecular Weight | 381.88 |
| Formula | C17H20ClN3O3S |
| Cas No. | 1215703-04-0 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 50 mg/mL (130.93 mM)  | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
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