Mexiletine (Synonyms: KOE-1173)

Name: Mexiletine
Brand: MedChemExpress
SKU: HY-119521
Rating: 5.0 (2 reviews)

Cat. No.: HY-119521 Purity: 99.92%: Data Sheet
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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

CAS No. : 31828-71-4

Size	Stock	Quantity
Liquid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Liquid
250 mg	In-stock	Estimated Time of Arrival: December 31
1 g	In-stock	Estimated Time of Arrival: December 31
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10 g	Get quote

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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Mexiletine:

2 Publications Citing Use of MCE Mexiletine

Featured Recommendations

•Related Screening Libraries:

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View All Sodium Channel Isoform Specific Products:

View All Isoforms

Na_v1.1 Na_v1.2 Na_v1.3 Na_v1.4 Na_v1.5 Na_v1.6 Na_v1.7 Na_v1.8 Na_v1.9

Biological Activity
Purity & Documentation
References
Customer Review

Description

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]

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	173 μM Compound: 36	Inhibition of of human TREK1 expressed in CHO cells assessed as reduction in channel currents Inhibition of of human TREK1 expressed in CHO cells assessed as reduction in channel currents	[PMID: 26588045]
CHO	IC₅₀	97.3 μM Compound: 36	Inhibition of of TASK1 (unknown origin) expressed in CHO cells assessed as reduction in channel currents Inhibition of of TASK1 (unknown origin) expressed in CHO cells assessed as reduction in channel currents	[PMID: 26588045]
HEK293	IC₅₀	11 μM Compound: 1, mexiletine	Blockade of human Nav1.7 channel expressed in HEK293 cells by FRET assay Blockade of human Nav1.7 channel expressed in HEK293 cells by FRET assay	[PMID: 18243692]
HEK293	IC₅₀	13 μM Compound: Mexiletine	Inhibition of human recombinant Nav1.5 channel expressed in HEK293 cells by whole cell voltage clamp technique Inhibition of human recombinant Nav1.5 channel expressed in HEK293 cells by whole cell voltage clamp technique	[PMID: 18501613]
HEK293	IC₅₀	2.9 μM Compound: Mexiletine	Inhibition of human recombinant Nav1.2 channel expressed in HEK293 cells by whole cell voltage clamp technique Inhibition of human recombinant Nav1.2 channel expressed in HEK293 cells by whole cell voltage clamp technique	[PMID: 18501613]
HEK293	IC₅₀	340 μM Compound: Mexiletine	Inhibition of fully inactivated human sodium channel Nav1.7 expressed in human HEK293 cells by patch-clamp electrophysiological assay Inhibition of fully inactivated human sodium channel Nav1.7 expressed in human HEK293 cells by patch-clamp electrophysiological assay	[PMID: 21634377]
HEK293	IC₅₀	420 μM Compound: Mexiletine	Blockade of human full-length NaV1.5 expressed in HEK293 cells co-transfected with pCD8-IRES-hbeta1 assessed as 0.1 Hz of half-maximal tonic-induced channel current at -120 mV holding potential after 36 to 72 hrs by patch clamp assay Blockade of human full-length NaV1.5 expressed in HEK293 cells co-transfected with pCD8-IRES-hbeta1 assessed as 0.1 Hz of half-maximal tonic-induced channel current at -120 mV holding potential after 36 to 72 hrs by patch clamp assay	[PMID: 22191686]
HEK293	IC₅₀	56 mM Compound: mexiletine	Antagonist activity at 20% inactivated human sodium channel Nav1.7 expressed in human HEK293 cells by patch-clamp electrophysiological assay Antagonist activity at 20% inactivated human sodium channel Nav1.7 expressed in human HEK293 cells by patch-clamp electrophysiological assay	[PMID: 22209205]
HEK293	IC₅₀	56 μM Compound: Mexiletine	Inhibition of human recombinant Nav1.8 channel expressed in HEK293 cells by whole cell voltage clamp technique Inhibition of human recombinant Nav1.8 channel expressed in HEK293 cells by whole cell voltage clamp technique	[PMID: 18501613]
HEK293	IC₅₀	56 μM Compound: Mexiletine	Inhibition of 20% inactivated human sodium channel Nav1.7 expressed in human HEK293 cells by patch-clamp electrophysiological assay Inhibition of 20% inactivated human sodium channel Nav1.7 expressed in human HEK293 cells by patch-clamp electrophysiological assay	[PMID: 21634377]
HEK293	IC₅₀	58 μM Compound: Mexiletine	Blockade of human full-length NaV1.5 expressed in HEK293 cells co-transfected with pCD8-IRES-hbeta1 assessed as 10 Hz of use-dependent-induced channel current at -120 mV holding potential after 36 to 72 hrs by patch clamp assay Blockade of human full-length NaV1.5 expressed in HEK293 cells co-transfected with pCD8-IRES-hbeta1 assessed as 10 Hz of use-dependent-induced channel current at -120 mV holding potential after 36 to 72 hrs by patch clamp assay	[PMID: 22191686]
HepG2	EC₅₀	2 mM Compound: Mexiletine	Cytotoxicity against human HepG2 cells assessed as cell viability after 2 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as cell viability after 2 hrs by MTT assay	[PMID: 22191686]
iPSC-CM	EC₅₀	1.8 μM Compound: 1	Antiarrhythmic activity in patient-derived hiPSC-CMs carrying LQT3 mutation assessed as shortening of action potential duration Antiarrhythmic activity in patient-derived hiPSC-CMs carrying LQT3 mutation assessed as shortening of action potential duration	[PMID: 33942619]
iPSC-CM	EC₅₀	20.4 μM Compound: 1	Antiarrhythmic activity in hiPSC-CMs assessed as prolongation of action potential Antiarrhythmic activity in hiPSC-CMs assessed as prolongation of action potential	[PMID: 33942619]

In Vitro

Mexiletine (10µM, 48 h) increases peak I_Na and late I_Na in HEK293A cells transfected with SCN5A-WT or SCN5A-1795insD while Mexiletine (10µM, 5 min) blocks the late I_Na^[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.

Molecular Weight

179.26

Formula

C₁₁H₁₇NO

CAS No.

31828-71-4

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
10 mM	0.5578 mL	2.7892 mL	5.5785 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.92%

Select Batch:

Data Sheet (275 KB) SDS (392 KB)

COA (247 KB) HNMR (237 KB) LCMS (88 KB)

Handling Instructions (2659 KB)

References

[1]. Campbell RW, et al. Mexiletine. N Engl J Med. 1987，316(1):29-34. [Content Brief]

[2]. De Bellis M, et al. Combined modifications of mexiletine pharmacophores for new lead blockers of Na(v)1.4 channels. Biophys J. 2013，104(2):344-54. [Content Brief]

[3]. Nasilli G, et al. Mexiletine reverses oxaliplatin-induced neuropathic pain in rats. J Pharmacol Sci. 2010;112(4):473-6. [Content Brief]

[4]. Egashira N, et al. Mexiletine reverses oxaliplatin-induced neuropathic pain in rats. J Pharmacol Sci. 2010，112(4):473-6. [Content Brief]

Complete Stock Solution Preparation Table

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

Mexiletine Related Classifications

Neurological Disease Cardiovascular Disease

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 (Synonyms: KOE-1173)

Customer Review

Other Forms of Mexiletine:

Mexiletine Related Antibodies

2 Publications Citing Use of MCE Mexiletine

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Sodium Channel Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Mexiletine Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Mexiletine Related Classifications

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