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Mexiletine hydrochloride

Name: Mexiletine hydrochloride
Brand: TargetMol
SKU: T1046
Price: 35 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T1046Cas No. 5370-01-4

Alias Mexiletine HCl, KOE-1173 (hydrochloride), KO1173

Mexiletine hydrochloride (KOE-1173 hydrochloride) is a voltage-gated sodium channel blocker and a Class IB antiarrhythmic drug. Mexiletine hydrochloride exerts antiarrhythmic effects by inhibiting sodium current in myocardial cells, thereby reducing the rise rate of cardiac action potential (phase 0) and reducing the automaticity of Purkinje fibers.

Mexiletine hydrochloride

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Purity: 99.88%

Catalog No. T1046Alias Mexiletine HCl, KOE-1173 (hydrochloride), KO1173Cas No. 5370-01-4

Pack Size	Price	USA Warehouse	Global Warehouse
50 mg	$35	In Stock	In Stock
100 mg	$48	In Stock	In Stock
200 mg	$59	In Stock	In Stock
500 mg	$68	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$50	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:99.88%

Color:White

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COA HNMR LCMS HPLC

Product Introduction

Mexiletine hydrochloride AI Summary

Mexiletine hydrochloride exhibits a diverse range of bioactivities. It demonstrates antiplasmodial activity against Plasmodium falciparum strains 7G8, GB4, and W2 with IC50 values of 12589.25 nM for 7G8 and GB4 and 6309.57 nM for W2. The compound also shows varying potency against other P. falciparum lines, including Dd2, ranging from 7079.5 nM to 12589.3 nM. Besides its antiplasmodial effects, Mexiletine hydrochloride is a potent modulator of Lamin A splicing with an IC50 of 11.2 nM and exhibits inhibitory activity against multiple targets such as GCN5L2, MPP8 Chromodomain, Histone Lysine Methyltransferase G9a, and Mammalian Selenoprotein Thioredoxin Reductase 1 with potencies ranging from 891.3 nM to 89125.1 nM. Additionally, it shows activity against Marburg Virus and Ebola Virus with AC50 values between 281.8 nM and 22.39 μM. In the context of sodium ion channels, Mexiletine hydrochloride inhibits NaV1.7, NaV1.1, and NaV1.5 in human and mouse models and provides analgesic effects in mice with an ED50 of 21.0 mg/kg, though it also reduces locomotor activity in mice with an ID50 of 45.0 mg/kg, yielding a therapeutic index of 2.1. The compound demonstrates limited efficacy against SARS-CoV-2 in Vero E6 cells with a low inhibition index of 0.1347 and exhibits moderate antifungal activity against Candida albicans (3.72%) but weak activity against Cryptococcus neoformans (-0.12%). Its antibacterial activity varies, showing inhibition percentages of 3.59% against E. coli, 13.5% against K. pneumoniae, 15.77% against P. aeruginosa, 22.29% against A. baumannii, and 13.57% against MRSA. In cardiovascular models, Mexiletine hydrochloride increases the arrhythmic threshold in guinea pig atria while exerting negative inotropic and chronotropic effects and inhibiting calcium-induced contractions in guinea pig aortic strips and smooth muscle. However, it also presents toxicity by impairing motor coordination in mice, with effects depending on the dosage and timing..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Mexiletine hydrochloride (KOE-1173 hydrochloride) is a voltage-gated sodium channel blocker and a Class IB antiarrhythmic drug. Mexiletine hydrochloride exerts antiarrhythmic effects by inhibiting sodium current in myocardial cells, thereby reducing the rise rate of cardiac action potential (phase 0) and reducing the automaticity of Purkinje fibers.
In vitro	Mexiletine shortened the cardiac Purkinje fiber effective response period (ERP) less than the action potential duration (APD), resulting in higher ERP/APD ratios.Mexiletine had no significant effect on atrioventricular conduction velocity, resting membrane potential, sinus node autoregulation, systolic arterial pressure, left ventricular function, or QRS or QT intervals. Mexiletine inhibits the inward flow of sodium ions through inhibition of sodium channels (requiring pulse initiation and conduction), which in turn reduces the rate of action potential elevation.
In vivo	Mexiletine shortened the cardiac Purkinje fiber effective response period (ERP) less than the action potential duration (APD), resulting in higher ERP/APD ratios.Mexiletine had no significant effect on atrioventricular conduction velocity, resting membrane potential, sinus node autoregulation, systolic arterial pressure, left ventricular function, or QRS or QT intervals. Mexiletine inhibits the inward flow of sodium ions through inhibition of sodium channels (requiring pulse initiation and conduction), which in turn reduces the rate of action potential elevation.
Synonyms	Mexiletine HCl, KOE-1173 (hydrochloride), KO1173

Chemical Properties

Molecular Weight	215.72
Formula	C₁₁H₁₈ClNO
Cas No.	5370-01-4
Smiles	Cl.CC(N)COc1c(C)cccc1C
Relative Density.	1.12 g/cm3

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 50 mg/mL (231.78 mM), Sonication is recommended.

H2O: 21.6 mg/mL (100.13 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (9.27 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

H2O/DMSO

	1mg	5mg	10mg	50mg
1 mM	4.6356 mL	23.1782 mL	46.3564 mL	231.7819 mL
5 mM	0.9271 mL	4.6356 mL	9.2713 mL	46.3564 mL
10 mM	0.4636 mL	2.3178 mL	4.6356 mL	23.1782 mL
20 mM	0.2318 mL	1.1589 mL	2.3178 mL	11.5891 mL
50 mM	0.0927 mL	0.4636 mL	0.9271 mL	4.6356 mL
100 mM	0.0464 mL	0.2318 mL	0.4636 mL	2.3178 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc