Celiprolol (hydrochloride)
(Synonyms: 盐酸塞利洛尔) 目录号 : GC12023A β1 adrenergic receptor antagonist
Cas No.:57470-78-7
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
Celiprolol is a β1 adrenergic receptor antagonist and β2 adrenergic receptor partial agonist.
β2 adrenergic receptor agonists, also known as adrenergic β2 receptor agonists, are a class of drugs acting on the β2 adrenergic receptor. Like other β adrenergic agonists, they cause smooth muscle relaxation.
In vitro: The ability of celiprolol to induce the regulation of beta adrenergic receptors was investigated in S49 lymphoma cells. Results showed that celiprolol did not stimulate adenylate cyclase in membranes from wild-type (WT) S49 cells or induced the sequestration of beta adrenergic receptors on intact cells. Moreover, exposure of WT S49 cells to celiprolol led to the loss of around half of the total cellular beta adrenergic receptors [1].
In vivo: In a previous study, Japanese white rabbits underwent 30 min of ischemia and 48 h of reperfusion. Celiprolol was administered 20 min before ischemia with or without pretreatment with N(omega)-nitro-L-arginine methylester (L-NAME) or 5-hydroxydecanoic acid sodium salt (5-HD). Results showed that celiprolol could significantly reduce the infarct size dose-dependently. The infarct size-reducing effect of celiprolol was found to be completely blocked by L-NAME but not by 5-HD. In addition, celiprolol could increase the myocardial interstitial levels of NOx and reduce the intensity of myocardium staining [2].
Clinical trial: In a previous clinical study, the authors suggested that celiprolol might be the treatment to prevent major complications in patients with vascular Ehlers-Danlos syndrome [3].
References:
[1] Reynolds EE, Molinoff PB. Down regulation of beta adrenergic receptors in S49 lymphoma cells induced by atypical agonists. J Pharmacol Exp Ther. 1986 Dec;239(3):654-60.
[2] Chen, X. ,Minatoguchi, S.,Arai, M., et al. Celiprolol, a selective β1-blocker, reduces the infarct size through production of nitric oxide in a rabbit model of myocardial infarction. Circulation Journal 71(4), 574-579 (2007).
[3] Ong KT et al. Effect of celiprolol on prevention of cardiovascular events in vascular Ehlers-Danlos syndrome: a prospective randomised, open, blinded-endpoints trial. Lancet. 2010 Oct 30;376(9751):1476-84.
| Cas No. | 57470-78-7 | SDF | |
| 别名 | 盐酸塞利洛尔 | ||
| 化学名 | N'-[3-acetyl-4-[3-[(1,1-dimethylethyl)amino]-2-hydroxypropoxy]phenyl]-N,N-diethyl-urea, monohydrochloride | ||
| Canonical SMILES | CC(C1=C(OCC(CNC(C)(C)C)O)C=CC(NC(N(CC)CC)=O)=C1)=O.Cl | ||
| 分子式 | C20H33N3O4 • HCl | 分子量 | 416.0 |
| 溶解度 | ≤2mg/ml in ethanol;10mg/ml in DMSO;10mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
| 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 | 2.4038 mL | 12.0192 mL | 24.0385 mL |
| 5 mM | 0.4808 mL | 2.4038 mL | 4.8077 mL |
| 10 mM | 0.2404 mL | 1.2019 mL | 2.4038 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。