| Size | Price | Stock | Qty |
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| 500mg |
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| 1g |
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| 2g |
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| 10g |
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| Other Sizes |
Purity: ≥98%
| Targets |
Mexiletine HCl targets voltage-gated sodium channels in cardiac cells. It acts as a non-selective voltage-gated sodium channel blocker. It inhibits the inward sodium current, reducing the rate of rise of the action potential (phase 0). It preferentially binds to open/inactivated channels. It has an IC50 of 75±8 µM for tonic block and 23.6±2.8 µM for use-dependent block. By stabilizing the neuronal membrane and reducing repetitive firing, it exerts antiarrhythmic effects.
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| ln Vitro |
Mexiletine is a local anesthetic, 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 channels. Mexiletine decreases the effective refractory period (ERP) in Purkinje fibers 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 vitro, Mexiletine HCl inhibits sodium channels with an IC50 of 75±8 µM for tonic block and 23.6±2.8 µM for use-dependent block. It is a voltage-gated sodium channel blocker. Its effects on sodium currents have been characterized in various cell-based assays. These in vitro studies confirm its mechanism as a sodium channel blocker and its antiarrhythmic potential. It is a class Ib antiarrhythmic agent. |
| ln 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 gastrointenstinal tract. |
| Enzyme Assay |
Non-cellular assays for Mexiletine HCl typically involve measuring its inhibition of sodium channel activity using purified channels or membrane preparations. These assays may use radioligand binding to assess its binding affinity for the sodium channel. Its effects on sodium currents can be measured using electrophysiological techniques in oocytes or other expression systems. These experiments are essential for characterizing its channel blocking properties.
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| Cell Assay |
In vitro cell-based assays for Mexiletine HCl are conducted using cardiac cells or cells expressing sodium channels to assess its effects on sodium currents. Patch-clamp electrophysiology is used to measure its effects on sodium currents. The compound's ability to inhibit the inward sodium current and reduce the rate of rise of the action potential is assessed. These experiments are crucial for confirming its mechanism of action.
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| Animal Protocol |
In vivo animal studies for Mexiletine HCl are typically conducted in animal models of cardiac arrhythmias to evaluate its antiarrhythmic efficacy. The compound is administered orally or intravenously, and its effects on cardiac electrophysiology are assessed. Electrocardiograms are recorded to measure changes in heart rate, rhythm, and conduction. These studies are essential for validating its in vivo efficacy as an antiarrhythmic agent.
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| ADME/Pharmacokinetics |
Mexiletine HCl has a molecular weight of 215.72 g/mol and a molecular formula of C11H17NO·HCl. It is an orally active compound. It is well-absorbed after oral administration and has a half-life that supports three-times-daily dosing. It is extensively metabolized in the liver and excreted in urine. Its pharmacokinetic properties are well-characterized. It is a prescription drug for ventricular arrhythmias.
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| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Medication Use During Lactation When mothers take up to 600 mg of mexiletine daily, the drug concentration in breast milk is low and no adverse effects are expected on breastfed infants. ◉ Effects on Breastfed Infants A 17-day-old breastfed infant experienced growth retardation, possibly related to the mother's use of mexiletine or atenolol (or both). The authors consider mexiletine unlikely to be the cause of the problem. A mother breastfed two infants after two pregnancies. The first infant was exposed to mexiletine for only 3 days at 9 months of age, with a breastfeeding rate of approximately 50%. The second infant was exposed to mexiletine via breast milk for 3 days at 3 months of age. All mothers received a dose of 200 mg three times daily. No adverse reactions were observed during the sampling period for both children. No adverse reactions were observed in mothers who started taking mexiletine at 10 months of age and breastfed their first 2-year-old child 3 to 5 times daily. ◉ Effects on breastfeeding and breast milk No published information found as of the revision date. Mexiletine HCl has an established safety profile from its clinical use. Common side effects include gastrointestinal disturbances, dizziness, and tremor. It can also cause neurological effects, such as paresthesia and ataxia. Comprehensive toxicological data are available from its clinical use. Mexiletine HCl is an approved antiarrhythmic drug. |
| References |
Curr Med Chem.2015;22(11):1400-13;Curr Pain Headache Rep.2010Apr;14(2):145-50.
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| Additional Infomation |
Mexiletine hydrochloride is the hydrochloride salt form of mexiletine, a local anesthetic and antiarrhythmic (Class IB) drug with a structure similar to lidocaine. Mexiletine exerts its antiarrhythmic effect by inhibiting inward sodium currents in cardiomyocytes, thereby reducing the rate of ascent of the myocardial action potential (phase 0) and decreasing the automaticity of Purkinje fibers. This slows nerve impulse conduction in the heart, stabilizing the heartbeat. The anesthetic effect of mexiletine stems from its ability to block the influx of sodium ions into peripheral nerves, thereby reducing the frequency and intensity of pain impulses reaching the central nervous system.
An antiarrhythmic drug with pharmacological effects similar to lidocaine. It may have some anticonvulsant effects. See also: Mexiletine (containing the active ingredient). Drug IndicationsNamuscla is indicated for the treatment of myotonic symptoms in adult patients with non-malnutritional myotonia. Treatment of Myotonia Mexiletine HCl (KOE-1173) is a class Ib antiarrhythmic agent that blocks voltage-gated sodium channels. It inhibits the inward sodium current, reducing the rate of rise of the cardiac action potential. It is used for the treatment of ventricular arrhythmias. Mexiletine HCl is an approved drug with a well-established clinical profile. |
| Molecular Formula |
C11H17NO.HCL
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| Molecular Weight |
215.72
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| Exact Mass |
215.107
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| CAS # |
5370-01-4
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| Related CAS # |
Mexiletine-d6 hydrochloride;1329835-60-0;Mexiletine-d3 hydrochloride
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| PubChem CID |
21467
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| Appearance |
White to off-white solid powder
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| Density |
0.979 g/cm3
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| Boiling Point |
271.5ºC at 760 mmHg
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| Melting Point |
200-203°C
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| Flash Point |
112.2ºC
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| LogP |
3.531
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
14
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| Complexity |
139
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
NFEIBWMZVIVJLQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H17NO.ClH/c1-8-5-4-6-9(2)11(8)13-7-10(3)12;/h4-6,10H,7,12H2,1-3H3;1H
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| Chemical Name |
1-(2,6-dimethylphenoxy)propan-2-amine hydrochloride
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (11.59 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (11.59 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (11.59 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (463.56 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.4636 mL | 2.3178 mL | 4.6356 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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