1. Membrane Transporter/Ion Channel
  2. Sodium Channel
  3. Mexiletine hydrochloride

Mexiletine hydrochloride  (Synonyms: KOE-1173 hydrochloride)

Cat. No.: HY-A0093 Purity: 99.92%
COA Handling Instructions

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 hydrochloride Chemical Structure

Mexiletine hydrochloride Chemical Structure

CAS No. : 5370-01-4

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Solid + Solvent
10 mM * 1 mL in DMSO
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Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Solid
100 mg USD 60 In-stock
500 mg USD 84 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Mexiletine hydrochloride:

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Mexiletine hydrochloride

  • 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.

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.
Clinical Trial
Molecular Weight

215.72

Formula

C11H18ClNO

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(N)COC1=C(C)C=CC=C1C.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 100 mg/mL (463.56 mM; Need ultrasonic)

DMSO : ≥ 41 mg/mL (190.06 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 4.6356 mL 23.1782 mL 46.3564 mL
5 mM 0.9271 mL 4.6356 mL 9.2713 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (11.59 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (11.59 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 100 mg/mL (463.56 mM); Clear solution; Need ultrasonic

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
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
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 (sealed storage, away from moisture). 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 / H2O 1 mM 4.6356 mL 23.1782 mL 46.3564 mL 115.8910 mL
5 mM 0.9271 mL 4.6356 mL 9.2713 mL 23.1782 mL
10 mM 0.4636 mL 2.3178 mL 4.6356 mL 11.5891 mL
15 mM 0.3090 mL 1.5452 mL 3.0904 mL 7.7261 mL
20 mM 0.2318 mL 1.1589 mL 2.3178 mL 5.7945 mL
25 mM 0.1854 mL 0.9271 mL 1.8543 mL 4.6356 mL
30 mM 0.1545 mL 0.7726 mL 1.5452 mL 3.8630 mL
40 mM 0.1159 mL 0.5795 mL 1.1589 mL 2.8973 mL
50 mM 0.0927 mL 0.4636 mL 0.9271 mL 2.3178 mL
60 mM 0.0773 mL 0.3863 mL 0.7726 mL 1.9315 mL
80 mM 0.0579 mL 0.2897 mL 0.5795 mL 1.4486 mL
100 mM 0.0464 mL 0.2318 mL 0.4636 mL 1.1589 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Mexiletine hydrochloride 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.

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Mexiletine hydrochloride
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