| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 25mg | |||
| Other Sizes |
| Targets |
Mexiletine D6 hydrochloride targets voltage-gated sodium channels, inhibiting the inward sodium current required for the initiation and conduction of impulses in the heart. This inhibition reduces the rate of rise of the action potential, stabilizing the cardiac membrane and preventing arrhythmias. As a deuterated analog of mexiletine hydrochloride, it retains the same pharmacological target and mechanism of action. The compound is a Class IB antiarrhythmic agent. Its molecular targets include voltage-gated sodium channels involved in cardiac action potential modulation.
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| ln Vitro |
In vitro, Mexiletine D6 hydrochloride is used to study the pharmacokinetics and metabolic pathways of mexiletine. As a deuterated form, it allows for precise tracking of the compound in biological systems. The compound is used in drug interaction studies to understand how mexiletine interacts with other drugs at the molecular level. It serves as an internal standard for LC-MS/MS-based quantitative bioanalysis of mexiletine in biological matrices. Its sodium channel blocking activity can be assessed in cell-based electrophysiology assays.
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| ln Vivo |
In vivo, Mexiletine D6 hydrochloride is used to study the pharmacokinetics and metabolic pathways of the parent compound due to its stable isotopic labeling. The deuterated form allows for precise tracking of the compound in biological systems. Mexiletine hydrochloride, the parent compound, is rapidly and completely absorbed after oral administration with oral bioavailability ranging from 80 to 88%. The compound is used in biological research related to cardiac arrhythmias and other medical conditions. Pharmacokinetic and metabolic studies are conducted in animal models.
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| Enzyme Assay |
Mexiletine D6 hydrochloride in vitro enzyme/receptor binding assays involve measuring voltage-gated sodium channel inhibition. Sodium channel activity is assessed using patch-clamp electrophysiology in cells expressing sodium channels. Binding affinity to sodium channels may be determined using radioligand binding displacement studies. For pharmacokinetic studies, the compound is used as an internal standard in LC-MS/MS assays for quantitative bioanalysis of mexiletine in biological matrices. Assays are performed in appropriate buffer systems with positive controls such as known sodium channel blockers (e.g., lidocaine).
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| Cell Assay |
Mexiletine D6 hydrochloride cell-based assays are conducted in cardiomyocytes or cells expressing voltage-gated sodium channels. Cells are cultured in appropriate media and treated with the compound at varying concentrations. Sodium channel activity is measured by patch-clamp electrophysiology to assess the inhibition of inward sodium current. For pharmacokinetic studies, cells are treated with the compound and intracellular concentrations are measured by LC-MS/MS. Cell viability is assessed by standard assays. Experiments are performed in triplicate with appropriate positive and negative controls.
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| Animal Protocol |
Mexiletine D6 hydrochloride in vivo studies are conducted in rodent models for pharmacokinetic and metabolic pathway analysis. Animals are administered the compound orally or via injection. Blood samples are collected at various time points for LC-MS/MS analysis to determine pharmacokinetic parameters such as Cmax, Tmax, half-life, and bioavailability. For metabolic pathway studies, urine and feces samples are collected for metabolite identification. Studies are conducted in accordance with institutional animal care guidelines.
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| ADME/Pharmacokinetics |
Mexiletine D6 hydrochloride (MW 221.76 g/mol, C11H12D6ClNO) is a deuterated small molecule. It is soluble in DMSO (50 mg/mL) and stable at 4°C sealed, away from moisture. The compound is a deuterium-labeled analog that offers enhanced stability and improved pharmacokinetic properties compared to the non-deuterated form. Pharmacokinetic parameters such as oral bioavailability (80-88% for the parent compound), half-life, and tissue distribution have been characterized for mexiletine.
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| Toxicity/Toxicokinetics |
Mexiletine D6 hydrochloride is generally well-tolerated in preclinical studies at doses used for pharmacokinetic research. The compound is a deuterated analog of mexiletine hydrochloride, a clinically used antiarrhythmic agent with established safety profiles. No significant adverse effects have been reported in the available literature at research-use concentrations. The compound is intended for research use only. Standard safety precautions should be followed when handling. Comprehensive toxicological evaluation is available from mexiletine clinical data.
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| References |
Curr Med Chem.2015;22(11):1400-13;Curr Pain Headache Rep.2010Apr;14(2):145-50. |
| Additional Infomation |
Mexiletine D6 hydrochloride is a deuterium-labeled analog of Mexiletine hydrochloride, a Class IB antiarrhythmic and non-selective voltage-gated sodium channel blocker. It is used as an internal standard for LC-MS/MS-based quantitative bioanalysis of mexiletine in biological matrices. The compound is used in pharmacokinetic studies, metabolic pathway analysis, and drug interaction studies. Its deuterated form enables precise tracking and enhanced stability for research applications. All applications are limited to non-human research use.
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| Molecular Formula |
C11H11D6NO.HCL
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|---|---|
| Molecular Weight |
221.757
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| Exact Mass |
221.145
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| CAS # |
1329835-60-0
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| Related CAS # |
Mexiletine hydrochloride;5370-01-4
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| PubChem CID |
71750725
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| Appearance |
White to off-white solid powder
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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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| SMILES |
[2H]C([2H])([2H])C([2H])(C([2H])([2H])OC1=C(C=CC=C1C)C)N.Cl
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| InChi Key |
NFEIBWMZVIVJLQ-SJPQGYSLSA-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/i3D3,7D2,10D;
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| Chemical Name |
1,1,1,2,3,3-hexadeuterio-3-(2,6-dimethylphenoxy)propan-2-amine;hydrochloride
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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. |
| 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) |
DMSO : ~50 mg/mL (~225.47 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.5094 mL | 22.5469 mL | 45.0938 mL | |
| 5 mM | 0.9019 mL | 4.5094 mL | 9.0188 mL | |
| 10 mM | 0.4509 mL | 2.2547 mL | 4.5094 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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