Flecainide acetate |
| Catalog No.GC15823 |
An inhibitor of cardiac late sodium current
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 54143-56-5
Sample solution is provided at 25 µL, 10mM.
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Flecainide, a nonselective Na (+) channel blocker, is a class 1C antiarrhythmic drug, especially used for the management of supraventricular arrhythmia. Flecainide has been used extensively in the effect on providing long-term sinus rhythm (SR) restoration as well as decreasing AF symptoms.
Flecainide revealed to suppress the Nav1.5 sodium channel in the heart, leading to prolongation of the cardiac action potential. Flecainide showed to reduce Ca+ spark, wave frequency and Ca+ wave velocity in the intact rat cardiomyocyte. Besides, flecainide has shown to reduce Ca(2+) wave when I(Na) is active. It has been demonstrated that flecainide could remarkably increase the Na(+)/Ca(2+)-exchanger (NCX)-mediated Ca(2+) efflux [1].
Flecainide has been reported to prolong ventricular repolarization, with the stronger effect at the left ventricular epicardium related to the right ventricular epicardium. Flecainide was found to produce a greater effective refractory period (ERP) lengthening at endocardium than epicardium, leading to a significant increase of ERP dispersion across the ventricular wall [2].
Flecainide has shown to dose-dependently reduce systemic pressures (32% at 0.8 μg/mL) and peripheral vascular resistance (15% at 0.8 μg/mL). In addition, at therapeutic plasma concentrations, flecainide at 0.8 μg/mL remarkably reduced the heart rate (55 beats/min) and increased QRS intervals (9.9 msec) in a rat hindlimb perfusion model [3].
References:
1.Sikkel MB1, Collins TP, Rowlands C, Shah M, O'Gara P, Williams AJ, Harding SE, Lyon AR, MacLeod KT. Flecainide reduces Ca(2+) spark and wave frequency via inhibition of the sarcolemmal sodium current. Cardiovasc Res. 2013 May 1;98(2):286-96. doi: 10.1093/cvr/cvt012. Epub 2013 Jan 19.
2.Osadchii OE.Flecainide-induced proarrhythmia is attributed to abnormal changes in repolarization and refractoriness in perfused guinea-pig heart. J Cardiovasc Pharmacol. 2012 Nov;60(5):456-66. doi: 10.1097/FJC.0b013e31826b86cf.
3.Allison B1, Yang Y, Pourrier M, Gibson JK. Comparison of the in vivo hemodynamic effects of the antiarrhythmic agents vernakalant and flecainide in a rat hindlimb perfusion model. J Cardiovasc Pharmacol. 2011 Apr;57(4):463-8. doi: 10.1097/FJC.0b013e318210276b.
| Cas No. | 54143-56-5 | SDF | |
| Chemical Name | acetic acid;N-(piperidin-2-ylmethyl)-2,5-bis(2,2,2-trifluoroethoxy)benzamide | ||
| Canonical SMILES | CC(=O)O.C1CCNC(C1)CNC(=O)C2=C(C=CC(=C2)OCC(F)(F)F)OCC(F)(F)F | ||
| Formula | C19H24F6N2O5 | M.Wt | 474.39 |
| Solubility | ≥ 47.4mg/mL in DMSO, ≥ 47.4mg/mL in EtOH, ≥ 23.7mg/mL in Water with ultrasonic and warming | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.108 mL | 10.5399 mL | 21.0797 mL |
| 5 mM | 421.6 μL | 2.108 mL | 4.2159 mL |
| 10 mM | 210.8 μL | 1.054 mL | 2.108 mL |
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μL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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