| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg |
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| Other Sizes |
| Targets |
Flecainide HCl targets cardiac sodium channels (Nav1.5), the rapid component of the delayed rectifier potassium channel (IKr), and the cardiac ryanodine receptor (RyR2). By blocking sodium channels, it reduces the rate of phase 0 depolarization and slows conduction in the heart. By inhibiting RyR2, it reduces spontaneous calcium release from the sarcoplasmic reticulum, which is relevant in CPVT. Its multiple mechanisms contribute to its antiarrhythmic effects.
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|---|---|
| ln Vitro |
In vitro, Flecainide HCl blocks cardiac sodium and potassium currents and inhibits RyR2-mediated calcium release. Specific IC₅₀ values for these targets are not provided in the available sources. Its effects on action potential duration have been characterized in isolated cardiac preparations.
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| ln Vivo |
In vivo, Flecainide HCl is used clinically as an antiarrhythmic agent. It is effective in suppressing various cardiac arrhythmias, including ventricular and supraventricular tachyarrhythmias. It has been studied in the context of CPVT, where it reduces arrhythmic events. Its efficacy has been established in clinical use.
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| Enzyme Assay |
A cell-free assay for Flecainide HCl would involve measuring its inhibition of sodium or potassium channel activity using patch-clamp techniques on isolated channels expressed in heterologous systems. Its inhibition of RyR2-mediated calcium release can be assessed using single-channel recordings or calcium flux assays with microsomal preparations. Specific IC₅₀ values are not provided.
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| Cell Assay |
Cellular assays for Flecainide HCl typically involve patch-clamp electrophysiology on cardiac myocytes or cell lines expressing cardiac sodium or potassium channels. The compound's ability to block these channels is measured by assessing changes in ionic currents. Its effects on calcium handling can be assessed in cells expressing RyR2. Specific protocols are not detailed in the available sources.
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| Animal Protocol |
In vivo animal experiments for Flecainide HCl are not described in the available sources. As a clinically used drug, its efficacy and safety have been established in human studies. Preclinical studies in animal models of arrhythmias likely contributed to its development, but specific protocols and data are not provided.
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| ADME/Pharmacokinetics |
Flecainide HCl is an orally active compound. It is well absorbed after oral administration. Its half-life is approximately 12-27 hours in humans, allowing for twice-daily dosing. It is metabolized in the liver, and its pharmacokinetics are influenced by CYP2D6 genotype. Specific PK parameters are not provided in the available sources.
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| Toxicity/Toxicokinetics |
Toxicity data for Flecainide HCl are not detailed in the available sources. As a clinically used drug, its safety profile is well established. Common adverse effects include dizziness, visual disturbances, and proarrhythmic effects. It is contraindicated in patients with structural heart disease due to the risk of proarrhythmia.
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| References | |
| Additional Infomation |
Flecainide HCl (CAS: 57415-44-8) is a potent, orally active antiarrhythmic agent classified as a Class IC agent. It blocks cardiac sodium channels, potassium channels, and the ryanodine receptor (RyR2). It is used in the treatment of various cardiac arrhythmias and is being studied for CPVT. Its molecular formula is C₁₇H₂₀F₆N₂O₃·HCl with a molecular weight of 450.80. It is available as an oral medication.
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| Molecular Formula |
C17H21CLF6N2O3
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|---|---|
| Molecular Weight |
450.803664922714
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| Exact Mass |
450.114
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| CAS # |
57415-44-8
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| Related CAS # |
Flecainide;54143-55-4
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| PubChem CID |
21447164
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| Appearance |
White to off-white solid powder
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| LogP |
4.962
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
29
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| Complexity |
500
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CCNC(C1)CNC(=O)C2=C(C=CC(=C2)OCC(F)(F)F)OCC(F)(F)F.Cl
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| InChi Key |
FPTQDMHWQWTIAX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H20F6N2O3.ClH/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;/h4-5,7,11,24H,1-3,6,8-10H2,(H,25,26);1H
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| Chemical Name |
N-(piperidin-2-ylmethyl)-2,5-bis(2,2,2-trifluoroethoxy)benzamide;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: ~100 mg/mL (~221.8 mM; with ultrasonication and warming by heating to 60°C)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.61 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 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 DMSO stock solution (20.8 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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 (4.61 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 DMSO stock solution (20.8 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. 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. Solubility in Formulation 3: ≥ 2.08 mg/mL (4.61 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 DMSO stock solution (20.8 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2183 mL | 11.0914 mL | 22.1828 mL | |
| 5 mM | 0.4437 mL | 2.2183 mL | 4.4366 mL | |
| 10 mM | 0.2218 mL | 1.1091 mL | 2.2183 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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