Cloperastine fendizoate
目录号: PL10019 纯度: ≥99%
CAS No. :85187-37-7
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中文名称
Cloperastine fendizoate
中文别名
氯苄哌醚联苯酰苯酸盐;氯哌斯汀Fendizoate;氯哌斯汀芬地柞酸盐;Cloperastine fendizoate
英文名称
Cloperastine fendizoate
英文别名
o-[(2'-hydroxy[1,1'-biphenyl]-4-yl)carbonyl]benzoic acid, compound with 1-[2-(4-chlorobenzhydryloxy)ethyl]piperidine (1:1);1-[2-[(4-chlorophenyl)-phenylmethoxy]ethyl]piperidine,2-(4-hydroxy-3-phenylbenzoyl)benzoic acid;Cloperastine Fendizoate
Cas No.
85187-37-7
分子式
C20H14O4.C20H24NOCl
分子量
648.19
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Cloperastine fendizoate 抑制 hERG K+ 电流,IC50 为 27 nM,这种作用具有浓度依赖性。
生物活性
Cloperastine fendizoate inhibits the hERG K currents in a concentration-dependent manner with an IC 50 value of 27 nM.
性状
Solid
IC50 & Target[1][2]
27 nM (K currents)
体外研究(In Vitro)
Cloperastine inhibits the hERG K currents in a concentrationdependent manner with IC50 value of 27±3 nM. 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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
In the anesthetized guinea pigs, Cloperastine at a therapeutic dose of 1 mg/kg prolonged the QT interval and monophasic action potential (MAP) duration without affecting PR interval or QRS width. 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 LD 50 in rats and mice for the two administration routes exceeds 1000 and 2000 mg/kg, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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.
溶解度数据
In Vitro: DMSO : 10 mg/mL (15.43 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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