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Cloperastine fendizoate
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。
Cloperastine fendizoate图片
CAS NO:85187-37-7
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
100mg电议

产品介绍
Cloperastinefendizoate抑制hERGK+电流,IC50为27nM,这种作用具有浓度依赖性。
Cas No.85187-37-7
别名氯苄哌醚联苯酰苯酸盐
Canonical SMILESO=C(O)C1=CC=CC=C1C(C2=CC(C3=CC=CC=C3)=C(O)C=C2)=O.ClC4=CC=C(C(C5=CC=CC=C5)OCCN6CCCCC6)C=C4
分子式C40H38ClNO5
分子量648.19
溶解度DMSO : ≥ 30 mg/mL (46.28 mM)
储存条件Store at -20°C
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

Cloperastine fendizoate inhibits the hERG K+ currents in a concentration-dependent manner with an IC50 value of 27 nM.

Cloperastine inhibits the hERG K+ currents in a concentrationdependent manner with IC50 value of 27±3 nM[1]. Among the antitussive agents, Cloperastine, which possesses antitussive and antiedemic activity, also relaxes the bronchial musculature. Cloperastine is a drug with a central antitussive effect, and is also endowed with an antihistaminic and papaverine-like activity similar to codeine but without its narcotic effects[2].

In the anesthetized guinea pigs, Cloperastine at a therapeutic dose of 1 mg/kg prolonged the QT interval and monophasicaction potential (MAP) duration without affecting PR interval or QRS width[1]. Cloperastine hydrochloride shows relatively low acute toxicity when administered by the intraperitoneal route in rats and mice, and shows minor toxicity by the oral route when administered as Cloperastine fendizoate, the LD50 in rats and mice for the two administration routes exceeds 1000 and 2000 mg/kg, respectively[2].

[1]. Takahara A, et al. Effects of the antitussive drug cloperastine on ventricular repolarization in halothane-anesthetized guinea pigs. J Pharmacol Sci. 2012;120(3):165-75. [2]. Catania MA, et al. Pharmacological and clinical overview of cloperastine in treatment of cough. Ther Clin Risk Manag. 2011;7:83-92.