Cloperastine-fendizoate - Potassium Channel 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECloperastine fendizoateCat. No.: HY-B2179CAS No.: 85187-37-7分式: CHClNO分量: 648.19作靶點(diǎn): Potassium Channel作通路: Membrane Transporter/Ion Channel儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 30

2、 mg/mL (46.28 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 1.5428 mL 7.7138 mL 15.4276 mL5 mM 0.3086 mL 1.5428 mL 3.0855 mL10 mM 0.1543 mL 0.7714 mL 1.5428 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Cloperastine fendizoate 抑制

3、 hERG K+ 電流，IC50 為 27 nM，這種作具有濃度依賴性。IC50 & Target 27 nM (K+ currents) 1體外研究Cloperastine inhibits the hERG K+ currents in a concentrationdependent manner with IC50 value of 273 nM1. Among the antitussive agents, Cloperastine, which possesses antitussive and antiedemic activity, also1/2 Master of Smal

4、l Molecules 您邊的抑制劑師www.MedChemErelaxes the bronchial musculature. Cloperastine is a drug with a central antitussive effect, and is alsoendowed with an antihistaminic and papaverine-like activity similar to codeine but without its narcotic effects2.體內(nèi)研究 In the anesthetized guinea pigs, Cloperastine a

5、t a therapeutic dose of 1 mg/kg prolonged the QT interval andmonophasicaction potential (MAP) duration without affecting PR interval or QRS width 1. Cloperastinehydrochloride shows relatively low acute toxicity when administered by the intraperitoneal route in rats andmice, and shows minor toxicity

6、by the oral route when administered as Cloperastine fendizoate, the LD50 inrats and mice for the two administration routes exceeds 1000 and 2000 mg/kg, respectively 2.REFERENCES1. Takahara A, et al. Effects of the antitussive drug cloperastine on ventricular repolarization in halothane-anesthetized guinea pigs. JPharmacol 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.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use onl