Mexiletine (Synonyms: KOE-1173)

Cat. No.: HY-119521: FAQs
Data Sheet Handling Instructions

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Mexiletine is an orally effective antiarrhythmic agent which has also been found to be effective for myotonia and neuropathic pain. Mexiletine exerts its efficacy through blocking sodium channels (IC₅₀ : 75±8 μM for tonic block, 23.6±2.8 μM for use-dependent block), therefore can be used for cardiovascular and neurological research.

For research use only. We do not sell to patients.

Mexiletine Chemical Structure

CAS No. : 31828-71-4

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Other In-stock Forms of Mexiletine:

Mexiletine hydrochloride

Other Forms of Mexiletine:

Mexiletine hydrochloride In-stock
Mexiletine-d₆ hydrochloride Get quote

1 Publications Citing Use of MCE Mexiletine

•Clin Chem. 2019 Dec;65(12):1522-1531. [Abstract]

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Na_v1.1 Na_v1.2 Na_v1.3 Na_v1.4 Na_v1.5 Na_v1.6 Na_v1.7 Na_v1.8

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

IC50: 75±8 μM for tonic block, 23.6±2.8 μM for use-dependent block (sodium channel of HEK293 transfected with hNav1.5 plasmid)^[2]

In Vitro

Mexiletine (10µM, 48 h) increases peak I_Na and late I_Na in HEK293A cells transfected with SCN5A-WT or SCN5A-1795insD while Mexiletine (10µM, 5 min) blocks the late I_Na^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Mexiletine (30, 100 mg/kg, p.o., acute administration) reverses both mechanical allodynia and cold hyperalgesia in Oxaliplatin (HY-17371) induced rats^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Sprague-Dawley rats with Oxaliplatin (HY-17371)-induced neuropathic pain ^[4]
Dosage:	Oxaliplatin (4 mg /kg) and Mexiletine(10, 30, 100 mg/kg)
Administration:	Oxaliplatin, Intraperitoneal injection (i.p.)in days 1, 2, 8, 9, 15, 16, 22, and 23; Mexiletine, Oral gavage (p.o.), acute administration
Result:	100 mg/kg completely reversed the reduction of 50% paw withdrawal threshold by Oxaliplatin at 60 min after administration in the von Frey test, completely reversed the increase of number of withdrawal responses at 60 and 120 min after administration in the acetone test. 30 mg/kg partly reversed the symptom and 10 mg/kg did not reverse any symptom. The effect disappeared by 180 min after administration.

Molecular Weight

179.26

Formula

C₁₁H₁₇NO

CAS No.

31828-71-4

SMILES

CC(COC1=C(C=CC=C1C)C)N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.

Protocol 1

PBS
Protocol 2

10% DMSO + 90% corn oil
Protocol 3

10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline
Protocol 4

10% DMSO + 90% (20% SBE-β-CD in saline)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Campbell RW, et al. Mexiletine. N Engl J Med. 1987，316(1):29-34. [Content Brief]

[2]. De Bellis M, et al. Combined modifications of mexiletine pharmacophores for new lead blockers of Na(v)1.4 channels. Biophys J. 2013，104(2):344-54. [Content Brief]

[3]. Nasilli G, et al. Mexiletine reverses oxaliplatin-induced neuropathic pain in rats. J Pharmacol Sci. 2010;112(4):473-6. [Content Brief]

[4]. Egashira N, et al. Mexiletine reverses oxaliplatin-induced neuropathic pain in rats. J Pharmacol Sci. 2010，112(4):473-6. [Content Brief]

Mexiletine Related Classifications

Neurological Disease Cardiovascular Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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