Name: Mexiletine hydrochloride - M115SM011 - M-115
Brand: Alomone Labs
SKU: M-115

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Overview

Cat #: M-115 Size: 1 g Lot: M115SM011

Alternative Name Ko 1173, Mexitil^®

Lyophilized Powder yes

Source Synthetic

MW: 215.7

Purity: >98%.

Effective concentration 10 μM – 2 mM.

Structure

Chemical name 1-(2,6-Dimethylphenoxy)-2-propanamine hydrochloride.

Molecular formula C₁₁H₁₇NO●HCl.

CAS No.: 5370-01-4

Activity Mexiletine is an orally effective antiarrhythmic drug of the IB class^1-4 with use-dependent Na⁺ channel-blocking properties^5-6, and it is used for the treatment of ventricular arrhythmia⁷. It is also among the few drugs used to reduce or prevent myotonia⁸. Mexiletine presents IC₅₀ values ranging from ~50 μM to ~100 μM and from ~20 μM to ~30 μM for tonic and phasic block, respectively, on single muscle fibers⁹ and a value of 253 μM in HEK293 cells¹⁰.

References-Activity

De Luca, A. et al. (2000) Mol. Pharmacol. 57, 268.
De Luca, A. et al. (1997) Naunyn Schmiedebergs Arch. Pharmacol. 356, 777.
De Luca, A. et al. (1997) J. Pharmacol Exp. Ther. 282, 93.
Fenster, P.E. and Comess, K.A. (1986) Pharmacotherapy 6, 1.
Lehmann-Horn, F. and Jurkat-Rott, K. (1999) Physiol. Rev. 79, 1317.
Jackson, C.E. et al. (1994) Muscle Nerve 17, 763.
Campbell, N.P. et al. (1978) Br. J. Clin. Pharmacol. 6, 103.
Cannon, S.C. (1996) Trends Neurosci. 19, 3.
Franchini, C. et al. (2003) J. Med Chem. 46, 5238.
Ruan, Y. et al. (2007) Circulation 116, 1137.

Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.

Solubility DMSO. Centrifuge all product preparations before use (10000 x g 5 min).

Storage of solutions Up to four weeks at 4°C or three months at -20°C.

Our bioassay

Alomone Labs Mexiletine hydrochloride inhibits Na_V1.4 channels heterologously expressed in Xenopus oocytes.
A. Time course of Na_V1.4 current amplitude changes as a result of 1 mM Mexiletine hydrochloride (#M-115) application (horizontal bar) for each of the two test pulses. B. Upper panel: Currents were elicited by a double test pulse protocol applied every 10 sec. For the first pulse the holding potential is -120 mV while the second pulse is preceded by 300 ms at 60 mV. Lower panel: Superimposed example current responses to the voltage stimulation before (black) and during application of 1 mM Mexiletine hydrochloride (green).

Scientific background

The clinical term myotonia is used to identify a series of dominant and recessive forms of genetic skeletal muscle diseases characterized by abnormal membrane excitability and delayed muscle relaxation after voluntary contraction. Sodium channel myotonias, paramyotonia congenita, and hyperkaliemic periodic paralysis are due to mutations of the gene coding for the skeletal muscle type of voltage-gated sodium channels^1,2.

Mexiletine, an orally effective antiarrhythmic drug of the IB class^3-6 with use-dependent sodium channel-blocking properties^2,7, is used for the treatment of ventricular arrhythmia⁸. Also, it is among the few drugs used to reduce or prevent myotonia^1,9-11, to treat long QT-3 syndrome¹² and to alleviate neuropathic pain¹³.

Mexiletine demonstrates IC₅₀ values ranging from ~50 μM to ~100 μM and from ~20 μM to ~30 μM for tonic and phasic block, respectively, on single muscle fibers¹⁴ and a value of 253 μM in HEK293 cells¹⁵.

Mexiletine has a neuroprotective feature against cerebral ischemia, spinal trauma and head trauma^5,16-20. In addition, it protects the neuronal tissue against diabetic oxidative damage²¹.

Target Na_V Na⁺ channels

Lyophilized Powder

For research purposes only, not for human use

Last Update: 30/03/2021

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