Mexiletine hydrochloride
Based on 2 publication(s) in Google Scholar
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.
- Purity: 99.88%
- CAS No.: 5370-01-4
- Formula: C11H18ClNO
- Molecular Weight:215.72
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Mexiletine hydrochloride
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Biological Activity
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]
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats with Oxaliplatin (HY-17371)-induced neuropathic pain [4]
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Dosage:Oxaliplatin (4 mg /kg) and Mexiletine(10, 30, 100 mg/kg)
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Administration:Oxaliplatin, Intraperitoneal injection (i.p.)in days 1, 2, 8, 9, 15, 16, 22, and 23; Mexiletine, Oral gavage (p.o.), acute administration
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 5370-01-4
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Appearance Solid
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Molecular Weight 215.72
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Formula C11H18ClNO
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Color White to off-white
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SMILES
CC(N)COC1=C(C)C=CC=C1C.[H]Cl
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Synonyms
KOE-1173 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (2)
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Journal Impact Factor
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Most Recent
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Clin Chem
Discovering Cross-Reactivity in Urine Drug Screening Immunoassays through Large-Scale Analysis of Electronic Health Records. [Abstract]2019 Dec;65(12):1522-1531. PMID: 31578215 -
Solvent & Solubility
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (463.56 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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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
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 |
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| 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.
Mexiletine hydrochloride Related Classifications
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