| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg | |||
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| Targets |
Flecainide acetate targets the voltage-gated sodium channel Nav1.5 in the heart. It binds to the sodium channel and inhibits the fast inward sodium current. This inhibition results in a decrease in the rate of rise of the action potential (phase 0), leading to a reduction in conduction velocity in the atria, ventricles, and His-Purkinje system. The drug stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses. Its action is use- and concentration-dependent.
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| ln Vitro |
Flecainide is a Class 1C antiarrhythmic medication intended only to treat arrhythmias of the supraventricular ventricle. Flecainide prolongs the heart's action potential by inhibiting the Nav1.5 sodium channels in the heart. In vitro: Without altering the resting membrane potential, flecainide (1-100 µM) extends the duration of action potentials in both early and late repolarization in a concentration-dependent manner under current-clamp conditions [1]. While flecainide inhibited WT and G1306E I(Na) similarly at a holding potential (HP) of -120 mV, it was more effective—depending on the R1448C channel. The holding voltage for WT must be more negative than the activation threshold in order to block to a higher extent than -120 and -180 mV [2]. In vivo: All eight patients' tachycardia was terminated by oral flecainide (80–130 mg/m(2)). One patient experienced an acute medication discontinuation due to oral flecainide loading, and another patient experienced a temporary medication discontinuation due to intravenous esmolol loading. Digoxin was given in two cases and propranolol was utilized in five cases as adjuvant therapy [3].
In vitro, Flecainide acetate inhibits the Nav1.5 sodium channel. Studies in rat cardiomyocytes have shown that flecainide reduces Ca2+ spark, wave frequency, and wave velocity. The compound's primary effect is to inhibit the fast sodium channel, which is responsible for the rapid upstroke of the myocardial action potential in cardiac conducting tissue. This action slows conduction and prolongs the refractory period. |
| ln Vivo |
In vivo, Flecainide acetate is used clinically as an antiarrhythmic agent. It has been used extensively for long-term sinus rhythm restoration and for decreasing atrial fibrillation symptoms. It is effective in managing supraventricular arrhythmias. By blocking the Nav1.5 sodium channel, it slows the upstroke of the cardiac action potential and reduces conduction velocity, thereby preventing and treating tachyarrhythmias.
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| Enzyme Assay |
The in vitro receptor binding assay for Flecainide acetate involves measuring its affinity for the Nav1.5 sodium channel using radioligand binding or electrophysiological techniques. For electrophysiology, cells expressing Nav1.5 are used in a patch-clamp configuration. The compound is applied at various concentrations (0.01-100 µM), and the inhibition of sodium current is measured. IC50 values are calculated from dose-response curves. Binding affinity can also be assessed using radiolabeled sodium channel blockers.
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| Cell Assay |
In vitro cellular assays for Flecainide acetate typically use cardiomyocytes or cell lines expressing Nav1.5. Cells are cultured and treated with the compound at various concentrations. The sodium current is measured using patch-clamp electrophysiology to determine the degree of channel block. Cell viability is assessed using MTT assays. The compound's effect on action potential parameters can be studied in isolated cardiac tissue preparations. These assays help characterize the compound's electrophysiological effects.
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| Animal Protocol |
In vivo animal studies for Flecainide acetate involve models of cardiac arrhythmia. The compound is administered orally or intravenously to animals, and the electrocardiogram (ECG) is monitored. The compound's ability to prevent or terminate induced arrhythmias is assessed. Its effects on heart rate, conduction intervals (PR, QRS, QT), and blood pressure are measured. Pharmacodynamic studies evaluate the relationship between drug concentration and its electrophysiological effects.
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| ADME/Pharmacokinetics |
Flecainide acetate has good oral bioavailability. It is well absorbed after oral administration and reaches therapeutic concentrations in the plasma. It is metabolized in the liver, primarily by CYP2D6, and its metabolites are excreted in the urine. The compound has a half-life of approximately 20 hours, allowing for twice-daily dosing. Its pharmacokinetics are affected by factors such as hepatic function and drug interactions. Flecainide acetate is a class Ic antiarrhythmic agent with the CAS number 54143-56-5. Its molecular formula is C17H20F6N2O3·C2H4O2. It is used to prevent and treat tachyarrhythmias. It works by blocking the Nav1.5 sodium channel in the heart. The compound is FDA-approved for clinical use and is available by prescription only.
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| References |
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| Additional Infomation |
Flecainide acetate is the acetate form of flecainide combined with an equimolar amount of acetic acid. It is an antiarrhythmic drug used to prevent and treat tachyarrhythmias (abnormally rapid heart rhythms). It is an antiarrhythmic drug containing the flecainide (1+) ion. Flecainide acetate is the acetate form of flecainide, a synthetic drug derived from trifluoroethoxybenzamide, possessing antiarrhythmic and local anesthetic activity. As a class Ic antiarrhythmic drug that blocks sodium channels, flecainide inhibits polarization phase 0 and reduces the induction rate of the His-Purkinje system. It also reduces the phase 4 slope and increases the depolarization threshold. A potent antiarrhythmic drug effective against a variety of ventricular and atrial arrhythmias and tachycardias. See also: Flecainide (containing the active ingredient).
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| Molecular Formula |
C19H24F6N2O5
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| Molecular Weight |
474.39500
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| Exact Mass |
474.158
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| CAS # |
54143-56-5
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| Related CAS # |
Flecainide-d4 acetate;1276197-21-7
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| PubChem CID |
41022
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| Appearance |
White to off-white solid powder
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| Density |
1.286g/cm3
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| Boiling Point |
434.9ºC at 760mmHg
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| Melting Point |
145-147℃
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| Flash Point |
216.8ºC
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| LogP |
4.251
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
32
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| Complexity |
531
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
RKXNZRPQSOPPRN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H20F6N2O3.C2H4O2/c18-16(19,20)9-27-12-4-5-14(28-10-17(21,22)23)13(7-12)15(26)25-8-11-3-1-2-6-24-11;1-2(3)4/h4-5,7,11,24H,1-3,6,8-10H2,(H,25,26);1H3,(H,3,4)
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| Chemical Name |
acetic acid;N-(piperidin-2-ylmethyl)-2,5-bis(2,2,2-trifluoroethoxy)benzamide
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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 (~105.40 mM)
H2O : ~20 mg/mL (~42.16 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.27 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 25.0 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: ≥ 2.5 mg/mL (5.27 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 25.0 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: ≥ 2.5 mg/mL (5.27 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 | 2.1079 mL | 10.5396 mL | 21.0793 mL | |
| 5 mM | 0.4216 mL | 2.1079 mL | 4.2159 mL | |
| 10 mM | 0.2108 mL | 1.0540 mL | 2.1079 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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