| 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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| Other Sizes |
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Flecainide acetate (Tambocor), the acetate salt form of flecainide, is a potent class Ic antiarrhythmic drug used in managing certain situations to prevent serious heart rhythm disorders or supraventricular arrhythmia. It works by blocking Nav1.5 sodium channels, which play a major part in the heart's electrical activity, thus causing prolongation of the cardiac action potential. When the heart is firing too quickly in an abnormal rhythm (arrhythmia), flecainide slows down the electricity to help the rhythm return to normal.
| 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].
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| References |
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| Additional Infomation |
Flecainide acetate is an acetate salt obtained by combining flecainide with one molar equivalent of acetic acid. An antiarrhythmic agent used to prevent and treat tachyarrhythmia (abnormal fast rhythm of the heart). It has a role as an anti-arrhythmia drug. It contains a flecainide(1+).
Flecainide Acetate is the acetate salt form of flecainide, a synthetic agent derived from trifluoroethoxy-benzamide exhibiting antiarrhythmic and local anesthetic activity. As a class Ic antiarrhythmic that blocks sodium channels, flecainide depresses polarization phase 0 and decreases the induction velocity of the His-Purkinje system. It also decreases phase 4 slope and increases the depolarization threshold. A potent anti-arrhythmia agent, effective in a wide range of ventricular and atrial ARRHYTHMIAS and TACHYCARDIAS. See also: Flecainide (has active moiety). |
| 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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