| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Targets |
The primary target of Tocainide hydrochloride is the voltage-gated sodium channel. It acts as a sodium channel blocker, specifically a class IB antiarrhythmic agent. By blocking sodium channels, it reduces the influx of sodium ions during the action potential, which decreases the excitability of cardiac muscle cells and suppresses abnormal electrical activity. It blocks the sodium channels in the pain-producing foci in the nerve membranes.
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| ln Vitro |
In vitro, Tocainide hydrochloride is a sodium channel blocker. Its activity is characterized by its ability to inhibit sodium currents in cardiac and neuronal cells. The compound's effects on action potential duration and conduction velocity can be assessed using electrophysiological techniques. These in vitro studies confirm its mechanism as a class IB antiarrhythmic agent.
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| ln Vivo |
In dogs with coronary artery blockage who are not under anesthesia, tocainide (100 mg/kg) significantly decreases ventricular ectopic activity. Ventricular ectopic activity recovered quickly after the tocainide infusion was stopped in models of coronary occlusion and digitalis toxicity [1].
In vivo, Tocainide hydrochloride is effective in suppressing ventricular arrhythmias. It is an orally effective antiarrhythmic agent, structurally and pharmacologically similar to lidocaine. It appears to be free of marked negative hemodynamic or electrophysiologic effects in patients with heart disease. The compound has also been used for the treatment of tinnitus. |
| Enzyme Assay |
In vitro receptor binding studies for Tocainide hydrochloride are not typical, as it acts on ion channels rather than receptors. Its activity is assessed using electrophysiological techniques, such as patch-clamp, to measure its inhibition of sodium currents in cells expressing voltage-gated sodium channels. The compound's potency and voltage-dependence are characterized in these assays.
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| Cell Assay |
In vitro cell-based assays for Tocainide hydrochloride evaluate its effects on cardiac or neuronal cell excitability. Cells are treated with the compound, and the action potential parameters are measured using microelectrode or patch-clamp techniques. The compound's ability to reduce the firing rate of neurons or to suppress abnormal electrical activity in cardiac cells is assessed.
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| Animal Protocol |
In vivo animal studies for Tocainide hydrochloride are conducted in models of cardiac arrhythmias. The compound is administered orally or intravenously, and its effects on cardiac rhythm are monitored using electrocardiography (ECG). Efficacy is assessed by measuring the suppression of induced arrhythmias. Pharmacokinetic studies determine the compound's absorption, distribution, metabolism, and excretion.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Tocainide hydrochloride have been characterized in preclinical and clinical studies. It is an orally active compound. In male Wistar rats, following oral administration of 15 mg/kg, about 15-20% of the dose administered was excreted as intact drug in the urine. An additional 20% of the dose was present as acid hydrolysable conjugates. The compound is metabolized to N-acetyl tocainide and other metabolites.
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| Toxicity/Toxicokinetics |
The toxicity profile of Tocainide hydrochloride includes a high frequency of minor and often transient central nervous system and gastrointestinal side effects. It appears to be free of marked negative hemodynamic or electrophysiologic effects in patients with heart disease. The compound is for research use only and is not intended for human therapeutic applications without proper authorization.
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| References |
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| Additional Infomation |
Tocainide hydrochloride is the hydrochloride form of tocainide, a primary amine analog of lidocaine with class 1b antiarrhythmic properties. Tocainide hydrochloride stabilizes neuronal membranes by reversibly binding to and blocking open and inactive voltage-gated sodium channels. This inhibits the inward sodium currents required to initiate and conduct impulses, and reduces the excitability of cardiomyocytes. The drug reduces the rate of rise and amplitude of action potentials in Purkinje fibers and myocardial fibers, and shortens the action potential duration (APD). Tocainide also shortens the effective refractory period (ERP) of Purkinje fibers, thereby increasing the ERP/APD ratio. Overall, these effects result in slowed nerve impulses and stabilized heart rate.
An antiarrhythmic drug that exerts a potential- and frequency-dependent blocking effect on sodium channels. Additional information: Tocainide hydrochloride is also known as 2-Amino-N-(2,6-dimethylphenyl)-propanamide Monohydrochloride. It is a voltage-gated sodium channel blocker. The compound is a primary amine analog of lidocaine. It has been used for the treatment of tinnitus and for suppressing ventricular arrhythmias. This product is for research use only and is not approved for clinical or therapeutic applications. |
| Molecular Formula |
C11H17CLN2O
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|---|---|
| Molecular Weight |
228.72
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| Exact Mass |
192.126
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| CAS # |
71395-14-7
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| Related CAS # |
Tocainide;41708-72-9
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| PubChem CID |
108173
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| Appearance |
Off-white to gray solid powder
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| LogP |
2.362
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
15
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| Complexity |
196
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=C(C(=CC=C1)C)NC(=O)C(C)N.Cl
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| InChi Key |
AMZACPWEJDQXGW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H16N2O.ClH/c1-7-5-4-6-8(2)10(7)13-11(14)9(3)12;/h4-6,9H,12H2,1-3H3,(H,13,14);1H
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| Chemical Name |
(1)-2-Amino-N-(2,6-dimethylphenyl)propionamide hydrochloride
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| Synonyms |
Alanyl-2,6-xylidide Astra W 36095 W36095 W 36095W-36095Tocainide 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 (e.g. under nitrogen), 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 : ~125 mg/mL (~546.52 mM)
H2O : ~50 mg/mL (~218.61 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (9.09 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 20.8 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: ≥ 2.08 mg/mL (9.09 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 20.8 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: ≥ 2.08 mg/mL (9.09 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.3722 mL | 21.8608 mL | 43.7216 mL | |
| 5 mM | 0.8744 mL | 4.3722 mL | 8.7443 mL | |
| 10 mM | 0.4372 mL | 2.1861 mL | 4.3722 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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