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Celiprolol(hydrochloride)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Celiprolol(hydrochloride)图片
CAS NO:57470-78-7
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
Celiprolol (REV 5320) 是一种强效、心脏选择性和口服活性的 β1-andrenoceptor r 拮抗剂,具有部分 β2 激动剂活性,Ki 值为 0.14-8.3 μM。
Cas No.57470-78-7
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 SMILESCC(C1=C(OCC(CNC(C)(C)C)O)C=CC(NC(N(CC)CC)=O)=C1)=O.Cl
分子式C20H33N3O4o 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℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.