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| Targets |
Modecainide targets fast voltage-gated sodium channels in cardiac myocytes. As a Class I antiarrhythmic agent, it binds to and blocks these sodium channels, thereby slowing the rapid influx of sodium ions during phase 0 depolarization of the cardiac action potential. This action reduces the excitability of ventricular myocytes and decreases conduction velocity, which helps suppress ventricular arrhythmias. Modecainide is a major metabolite of Encainide, and its antiarrhythmic activity is attributed to its interaction with cardiac sodium channels. The compound's mechanism is similar to that of lidocaine and other Class I antiarrhythmics, making it a useful reference compound in cardiovascular electrophysiology research focused on sodium-channel blockade and antiarrhythmic drug mechanisms.
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| ln Vitro |
In vitro studies have demonstrated that Modecainide effectively blocks fast voltage-gated sodium channels in cardiac myocytes. By slowing phase 0 depolarization, the compound reduces the excitability and conduction velocity of ventricular myocytes. Modecainide is a major metabolite of Encainide, and studies have evaluated the effects of Encainide and its two major metabolites-O-demethylated Encainide (MJ 9444) and 3-O-methoxy Encainide (MJ 14030, Modecainide)-on cardiac electrophysiology. The compound's in vitro activity is characterized by its ability to suppress abnormal electrical activity in cardiac tissue, making it effective against ventricular arrhythmias. Modecainide's potency in slowing conduction and reducing excitability has been confirmed in various electrophysiological preparations.
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| ln Vivo |
O-desmethylated encainide (MJ 9444) and 3-O-Effects of methoxyencainide (MJ 14030) on cardiac conduction in canine hearts following atrioventricular node disruption in vivo are the two main metabolites of encainib. When it came to decreasing conduction in the rabbit heart's atria, atrioventricular nodes, and His-Purkinje system, both metabolites were 4–15 times more effective than encainide. Encainide (0.8-3.2 mg/kg iv) prolongs the effective and functional refractory periods of the Purkinje pathway in dogs while slowing Purkinje and muscle presystolic conduction at all coupled intervals. Without altering or concurrently slowing down the conduction of late beats (more than 350 msec), MJ 9444 (0.05-0.4 mg/kg) quickens the Purkinje conduction of premature beats (less than 300 msec). Increased dosages (0.4–1.6 mg/kg) cause conduction to slow down constantly. Although in some cases the effective and functional refractory times recovered to control values at larger doses, they were nonetheless shortened. At dosages of 0.4 mg/kg or above, muscle conduction is delayed. The effects of MJ 14030 (0.05-3.2 mg/kg) were not consistent; in three studies, it behaved like MJ 9444, but in two more, it behaved like the parent drug [1].
In vivo studies have shown that Modecainide, as a major metabolite of Encainide, contributes to the antiarrhythmic effects observed following Encainide administration. Studies have evaluated the effects of Encainide and its two major metabolites, O-demethylated Encainide (MJ 9444) and 3-O-methoxy Encainide (Modecainide, MJ 14030), in animal models. Modecainide has been investigated in preclinical and limited clinical studies for its potential to treat ventricular tachycardia and other life-threatening rhythm disturbances. The compound's ability to slow phase 0 depolarization in ventricular myocytes and reduce conduction velocity has been demonstrated in vivo. Although not widely adopted therapeutically, Modecainide remains a useful reference compound in cardiovascular electrophysiology research. |
| Enzyme Assay |
The in vitro enzyme/receptor binding assay for Modecainide typically involves measuring its inhibitory effect on fast voltage-gated sodium channels in cardiac myocytes using electrophysiological techniques. The assay system commonly uses isolated cardiac myocytes or heterologous expression systems (such as HEK293 cells) expressing cardiac sodium channel isoforms (Nav1.5). Patch-clamp electrophysiology in whole-cell configuration is used to record sodium currents before and after application of Modecainide at varying concentrations (typically 0.1-100 uM). The compound's effect on peak sodium current, steady-state inactivation, and use-dependent block is assessed. Alternatively, radioligand binding assays using [3H]batrachotoxin or other sodium channel ligands can be employed to assess binding affinity. Assay buffer typically contains HEPES, sodium chloride, calcium chloride, and potassium chloride at physiological pH.
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| Cell Assay |
The in vitro cell-based assay for Modecainide involves culturing relevant cell lines such as cardiac myocytes (e.g., HL-1 cells, primary neonatal rat ventricular myocytes) or HEK293 cells expressing cardiac sodium channels. Cells are typically seeded in multi-well plates or on coverslips and treated with varying concentrations of Modecainide (0.1-100 uM) for 1-24 hours in appropriate culture media at 37degC with 5% CO2. Following treatment, electrophysiological properties are assessed using patch-clamp recording to measure sodium channel activity and action potential parameters. Cell viability can be assessed using standard assays such as MTT or LDH release. Additionally, the compound's effects on cardiac conduction can be evaluated using multi-electrode array (MEA) systems to measure field potential duration and conduction velocity in cardiac cell monolayers.
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| Animal Protocol |
In vivo animal studies for Modecainide have been conducted as part of the characterization of Encainide and its metabolites. Studies have evaluated the effects of Encainide and its two major metabolites, O-demethylated Encainide (MJ 9444) and 3-O-methoxy Encainide (Modecainide, MJ 14030), in animal models of cardiac arrhythmias. Typical animal models include rodents (rats, mice) or larger animals (dogs, rabbits) with induced arrhythmias. Modecainide is administered via intravenous or intraperitoneal routes at doses determined based on preliminary pharmacokinetic data. Common endpoints include electrocardiographic monitoring (PR interval, QRS duration, QT interval), assessment of arrhythmia suppression, and evaluation of hemodynamic parameters. The compound's ability to slow conduction and suppress ventricular arrhythmias has been demonstrated in these studies.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Modecainide have been studied as part of the characterization of Encainide metabolism. Modecainide (MJ 14030) is a major metabolite of Encainide formed through O-demethylation. The compound has a molecular weight of 368.47 g/mol and a molecular formula of C22H2₈N2O3. Its chemical structure is 4-hydroxy-3-methoxy-N-[2-[2-(1-methylpiperidin-2-yl)ethyl]phenyl]benzamide. The compound is soluble in DMSO and has a purity of ≥95%. As a metabolite of Encainide, Modecainide's pharmacokinetic profile is influenced by the parent drug's metabolism and distribution. However, detailed pharmacokinetic parameters such as half-life, bioavailability, and clearance have not been extensively reported in the available literature.
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| Toxicity/Toxicokinetics |
Modecainide (CAS#: 81329-71-7) is a research-grade antiarrhythmic compound with the molecular formula C22H2₈N2O3 and a molecular weight of 368.47. Also known as MJ 14030 and BMY 40327, Modecainide is a major pharmacologically active metabolite of the Class IC antiarrhythmic agent Encainide. As a Class I antiarrhythmic agent structurally related to lidocaine, Modecainide blocks fast voltage-gated sodium channels, slowing phase 0 depolarization in ventricular myocytes and reducing excitability and conduction velocity. The compound has been investigated in preclinical and limited clinical studies for its potential to treat ventricular tachycardia and other life-threatening rhythm disturbances. Although not widely adopted therapeutically, it remains a useful reference compound in cardiovascular electrophysiology research. The compound has a purity of ≥95% and is intended for research purposes only. No current clinical approvals have been reported.
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| References | |
| Additional Infomation |
Modecainide belongs to the phenolic class of compounds and also to the methoxybenzene class of compounds.
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| Molecular Formula |
C₂₂H₂₈N₂O₃
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| Molecular Weight |
368.47
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| Exact Mass |
368.21
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| CAS # |
81329-71-7
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| PubChem CID |
54737
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| Appearance |
White to off-white solid powder
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| Density |
1.162g/cm3
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| Boiling Point |
480.6ºC at 760 mmHg
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| Flash Point |
244.4ºC
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| Index of Refraction |
1.598
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| LogP |
4.391
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
27
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| Complexity |
473
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(NC1=CC=CC=C1CCC2N(C)CCCC2)C3=CC=C(O)C(OC)=C3
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| Synonyms |
MJ 14030; BMY 40327
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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 |
| 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) |
Methanol :≥ 250 mg/mL (~678.48 mM)
DMSO : ~100 mg/mL (~271.39 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 | 2.7139 mL | 13.5696 mL | 27.1393 mL | |
| 5 mM | 0.5428 mL | 2.7139 mL | 5.4279 mL | |
| 10 mM | 0.2714 mL | 1.3570 mL | 2.7139 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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