Home Transmembrane Transporters Sodium Channel inhibitor Mexiletine HCl

Mexiletine HCl

Catalog No.S4225 Synonyms: KO1173

For research use only.

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

Mexiletine HCl Chemical Structure

CAS No. 5370-01-4

Selleck's Mexiletine HCl has been cited by 1 Publication

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Biological Activity

Description Mexiletine HCl (KO1173) belongs to Class IB anti-arrhythmic group of medicines, inhibits sodium channels to reduce the inward sodium current.
Targets
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]

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 215.72
Formula

C11H17NO.HCl
CAS No. 5370-01-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(C(=CC=C1)C)OCC(C)N.Cl

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04622553 Recruiting Drug: Mexiletine Myotonic Disorders Lupin Ltd. November 3 2021 Not Applicable
NCT04700046 Not yet recruiting Drug: Mexiletine 167 mg|Drug: Placebo Myotonic Dystrophy Type 1 and Type 2 Lupin Ltd. July 6 2021 Phase 3
NCT02045667 Completed Drug: Mexiletine|Drug: Placebo Non Dystrophic Myotonia Radboud University|ZonMw: The Netherlands Organisation for Health Research and Development January 2014 Phase 2
NCT01849770 Completed Drug: Mexiletine|Drug: Placebo Sporadic Amyotrophic Lateral Sclerosis University of Washington July 2013 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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