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Mexiletine HCl Sodium Channel inhibitor

Cat.No.S4225

Mexiletine HCl (KO1173,Mexitil) belongs to Class IB anti-arrhythmic group of medicines, inhibits sodium channels to reduce the inward sodium current.
Mexiletine HCl Sodium Channel inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 215.72

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Chemical Information, Storage & Stability

Molecular Weight 215.72 Formula

C11H17NO.HCl

 Storage (From the date of receipt)
CAS No. 5370-01-4 Download SDF Storage of Stock Solutions

Synonyms KO1173,Mexitil Smiles CC1=C(C(=CC=C1)C)OCC(C)N.Cl

Solubility

In vitro
Batch:

DMSO : 43 mg/mL (199.33 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 43 mg/mL

Ethanol : 43 mg/mL

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
Sodium channel [1]
In vitro

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. [1]
In vivo

Mexiletine 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. [2]
References

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