2. Membrane Transporter/Ion Channel
  3. Sodium Channel
  4. Mexiletine

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

Mexiletine Chemical Structure

CAS No. : 31828-71-4

Size Price Stock Quantity
Liquid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
Liquid
250 mg In-stock
1 g In-stock
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10 g   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Mexiletine:

Mexiletine Related Antibodies

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1 Publications Citing Use of MCE Mexiletine

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2][3][4][5].

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

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

Mexiletine Related Antibodies
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.
Appearance

Liquid

Color

Colorless to light yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 175 mg/mL (976.24 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 5.5785 mL 27.8924 mL 55.7849 mL
5 mM 1.1157 mL 5.5785 mL 11.1570 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
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Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

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
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 5.5785 mL 27.8924 mL 55.7849 mL 139.4622 mL
5 mM 1.1157 mL 5.5785 mL 11.1570 mL 27.8924 mL
10 mM 0.5578 mL 2.7892 mL 5.5785 mL 13.9462 mL
15 mM 0.3719 mL 1.8595 mL 3.7190 mL 9.2975 mL
20 mM 0.2789 mL 1.3946 mL 2.7892 mL 6.9731 mL
25 mM 0.2231 mL 1.1157 mL 2.2314 mL 5.5785 mL
30 mM 0.1859 mL 0.9297 mL 1.8595 mL 4.6487 mL
40 mM 0.1395 mL 0.6973 mL 1.3946 mL 3.4866 mL
50 mM 0.1116 mL 0.5578 mL 1.1157 mL 2.7892 mL
60 mM 0.0930 mL 0.4649 mL 0.9297 mL 2.3244 mL
80 mM 0.0697 mL 0.3487 mL 0.6973 mL 1.7433 mL
100 mM 0.0558 mL 0.2789 mL 0.5578 mL 1.3946 mL
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Mexiletine Related Classifications

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.

Keywords:

Mexiletine31828-71-4KOE-1173KOE1173KOE 1173Sodium ChannelNa channelsNa+ channelsantiarrhythmic agentmyotonianeuropathic painsodium channelcardiovascularneurologicalHEK293AhiPSC-CMsSprague-Dawley ratsInhibitorinhibitorinhibit

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