Celiprolol(hydrochloride)

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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。

CAS NO:

57470-78-7

包装与价格：

包装	价格(元)
5mg	询价
10mg	询价
25mg	询价

化学性质

Physical Appearance	A crystalline solid
Storage	Store at -20°C
M.Wt	416
Cas No.	57470-78-7
Formula	C₂₀H₃₃N₃O₄·HCl
Synonyms	Corliprol,NSC 324509
Solubility	≤2mg/ml in ethanol;10mg/ml in DMSO;10mg/ml in dimethyl formamide
Chemical Name	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
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

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.