BMS 182874 hydrochloride
目录号 : GC15537
ETA antagonist
Cas No.:1215703-04-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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:
[1] MARIA L WEBB, J. EILEEN BIRD, EDDIE C. K. LIU, PATRICIA M. ROSE, RANDY SERAFINO, PHILIP D. STEIN and SUZANNE MORELAND. BMS-182874 is a selective, nonpeptide endothelin ETA receptor antagonist. JPET 272:1124-1134, 1995.
| Cas No. | 1215703-04-0 | SDF | |
| 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 | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6186 mL | 13.0931 mL | 26.1862 mL |
| 5 mM | 0.5237 mL | 2.6186 mL | 5.2372 mL |
| 10 mM | 0.2619 mL | 1.3093 mL | 2.6186 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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