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Mexiletine HCl Sodium Channel inhibitor

Name: Mexiletine HCl
Brand: Selleck Chemicals
SKU: S4225
Rating: 5 (2 reviews)

Cat.No.S4225

Mexiletine HCl (KO1173, Mexitil) belongs to Class IB anti-arrhythmic group of medicines, inhibits Sodium Channel to reduce the inward sodium current.

Chemical Structure

Molecular Weight: 215.72

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Quality Control

Batch: Purity: 99.96%

99.96

Related Targets	CFTR CRM1 CD markers AChR Calcium Channel Potassium Channel GABA Receptor TRP Channel ATPase GluR
Other Sodium Channel Inhibitors	Camostat Mesilate A-803467 cariporide Tolperisone HCl Vinpocetine Veratramine Bulleyaconi cine A Ambroxol HCl Benzocaine Nefopam HCl

Chemical Information, Storage & Stability

Molecular Weight	215.72	Formula	C₁₁H₁₇NO.HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	5370-01-4	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	KO1173,Mexitil			Smiles	CC1=C(C(=CC=C1)C)OCC(C)N.Cl

Solubility

In vitro
Batch:

DMSO : 43 mg/mL (199.33 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 43 mg/mL

Ethanol : 43 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	Sodium channel
In vitro	Mexiletine is a local anaesthetic, antiarrhythmic agent (Class Ib), structurally similar to lidocaine, but orally active. Mexiletine, inhibits the inward sodium current required for the initiation and conduction of impulses, thus reducing the rate of rise of the action potential. It achieves this reduced sodium current by inhibiting Sodium Channel. Mexiletine decreases the effective refractory period (ERP) in Purkinje fibres in the heart. The decrease in ERP is of lesser magnitude than the decrease in action potential duration (APD), which results in an increase in the ERP/APD ratio. It does not significantly affect resting membrane potential or sinus node automaticity, left ventricular function, systolic arterial blood pressure, atrioventricular (AV) conduction velocity, or QRS or QT intervals.
In vivo	Mexiletine has fast onset and offset kinetics, meaning that they have little or no effect at slower heart rates, and more effects at faster heart rates. It shortens the action potential duration, reduces refractoriness, and decreases Vmax in partially depolarized cells with fast response action potentials. Mexiletine either does not change the action potential duration, or decreases the action potential duration. Mexiletine is well absorbed (bioavailability 90%) from the gastrointestinal tract.
References	[1] http://en.wikipedia.org/wiki/Mexiletine [2] http://dailymed.nlm.nih.gov/

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