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Mexiletine HCl(KOE-1173)
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。
Mexiletine HCl(KOE-1173)图片
CAS NO:5370-01-4
规格:≥98%
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议
1g电议
2g电议
10g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)215.72
FormulaC11H17NO.HCl
CAS No.5370-01-4
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 43 mg/mL (199.3 mM)
Water: 43 mg/mL (199.3 mM)
Ethanol: 43 mg/mL (199.3 mM)
Other info

Chemical Name: 1-(2,6-dimethylphenoxy)propan-2-amine hydrochloride

InChi Key: NFEIBWMZVIVJLQ-UHFFFAOYSA-N

InChi Code: InChI=1S/C11H17NO.ClH/c1-8-5-4-6-9(2)11(8)13-7-10(3)12;/h4-6,10H,7,12H2,1-3H3;1H

SMILES Code: CC(N)COC1=C(C)C=CC=C1C.[H]Cl

SynonymsKO1173; Mexiletine, Mexitil, Mexiletene, KO-1173, KO 1173
实验参考方法
In Vitro

In vitro activity: Mexiletine is a local anesthetic, antiarrhythmic agent (Class Ib), structurally similar to lidocaine, but orally active. Mexiletine, inhibits the inward sodium current required for the initiation and conduction of impulses, thus reducing the rate of rise of the action potential. It achieves this reduced sodium current by inhibiting sodium channels. Mexiletine decreases the effective refractory period (ERP) in Purkinje fibers in the heart. The decrease in ERP is of lesser magnitude than the decrease in action potential duration (APD), which results in an increase in the ERP/APD ratio. It does not significantly affect resting membrane potential or sinus node automaticity, left ventricular function, systolic arterial blood pressure, atrioventricular (AV) conduction velocity, or QRS or QT intervals

In VivoMexiletine has fast onset and offset kinetics, meaning that they have little or no effect at slower heart rates, and more effects at faster heart rates. It shortens the action potential duration, reduces refractoriness, and decreases Vmax in partially depolarized cells with fast response action potentials. Mexiletine either does not change the action potential duration, or decreases the action potential duration. Mexiletine is well absorbed (bioavailability 90%) from the gastrointenstinal tract.
Animal model
Formulation & Dosage
References

Curr Med Chem. 2015;22(11):1400-13; Curr Pain Headache Rep. 2010 Apr;14(2):145-50.