| CAS NO: | 1215703-04-0 |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 50mg | 电议 |
| Cas No. | 1215703-04-0 |
| 化学名 | 5-(dimethylamino)-N-(3,4-dimethylisoxazol-5-yl)naphthalene-1-sulfonamide hydrochloride |
| Canonical SMILES | CC(C(C)=NO1)=C1NS(C2=CC=CC3=C2C=CC=C3N(C)C)(=O)=O.Cl |
| 分子式 | C17H19N3O3S.HCl |
| 分子量 | 381.88 |
| 溶解度 | Soluble to 100 mM in DMSO |
| 储存条件 | Store at RT |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Ki: 61 nM for ETA in VSM-A10 cells; 48 nM for ETA in CHO cells Endothelin (ET) was originally identified as a potent vasoactive substance secreted by endothelial cells that stimulated force development in isolated pig coronary arteries. ET-1 belongs to a family of highly conserved 21-amino-acid peptides produced in numerous tissues including the lung, kidney, eye, gut and central nervous system. BMS-182874 is a low molecular weight, nonpeptide endothelin (El) receptor antagonist. In vitro: 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. 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 [1]. In vivo: When administered either orally (ED50 = 30 μmol/kg) or intravenously (ED50 = 24 μmol/kg) to conscious, normotensive rats, BMS-182874 blunted the pressor response to exogenous ET-l . These data demonstrate that BMS-l 82874 is a competitive, selective and orally active ETA receptor antagonist [1]. Clinical trial: Up to now, BMS 182874 hydrochloride is still in the preclinical development stage. Reference: |
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