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> Flecainide (acetate) [54143-56-5]

Flecainide (acetate) [54143-56-5]

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Flecainide acetate (R-818) is a class 1C antiarrhythmic agent especially used for the management of supraventricular arrhythmia; works by blocking the Nav1.5 sodium channel in the heart, causing prolongation of the cardiac action potential.

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Flecainide acetate Estructura química

Flecainide acetate Estructura química

No. CAS : 54143-56-5

This product is a controlled substance and not for sale in your territory.

Based on 1 publication(s) in Google Scholar

Other Forms of Flecainide acetate:

  • Flecainide-d4 acetate Obtener un presupuesto
  • Flecainide Obtener un presupuesto
  • Flecainide hydrochloride Obtener un presupuesto
  • Flecainide acetate (Standard) Obtener un presupuesto

Ver todos los productos específicos de isoformas Sodium Channel:

Ver todas las isoformas
Nav1.1 Nav1.2 Nav1.3 Nav1.4 Nav1.5 Nav1.6 Nav1.7 Nav1.8
Descripciòn

Flecainide acetate (R-818) is a class 1C antiarrhythmic agent especially used for the management of supraventricular arrhythmia; works by blocking the Nav1.5 sodium channel in the heart, causing prolongation of the cardiac action potential.

IC50 & Target[1]

Nav1.5

 

In Vitro

Flecainide is a class 1C antiarrhythmic drug especially used for the management of supraventricular arrhythmia. Flecainide works by blocking the Nav1.5 sodium channel in the heart, causing prolongation of the cardiac action potential. in vitro: Under the current-clamp condition, flecainide (1-100 microM) prolonged the action potential duration at both the early and the late phases of repolarization in a concentration-dependent manner without affecting the resting membrane potential [1]. At a holding potential (HP) of -120 mV, flecainide use-dependently blocked WT and G1306E I(Na) equally but was more potent on R1448C channels. For WT, the extent of block depended on a holding voltage more negative than the activation threshold, being greater at -90 mV as compared to -120 and -180 mV [2]. in vivo: Flecainide (80-130 mg/m(2) orally) resulted in termination of the tachycardia in all 8 patients. Acute pharmacological termination of arrhythmia occurred with oral flecainide loading in 1 and temporarily with intravenous esmolol loading in 1 patient. Adjuvant therapy in form of propranolol was used in 5 and digoxin in 2 [3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Flecainide acetate Related Antibodies
Ensayo clínico
Peso molecular

474.39

Fòrmula

C19H24F6N2O5
No. CAS

54143-56-5
Appearance

Solid

Color

White to off-white

SMILES

O=C(NCC1NCCCC1)C2=CC(OCC(F)(F)F)=CC=C2OCC(F)(F)F.CC(O)=O
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvente y solubilidad
In Vitro: 

DMSO : 50 mg/mL (105.40 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 20 mg/mL (42.16 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1080 mL 10.5399 mL 21.0797 mL
5 mM 0.4216 mL 2.1080 mL 4.2159 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Calculadora de molaridad

  • Calculadora de dilución

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.27 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.27 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Pureza y Documentación
Referencias

  • [1]. Yamashita T, Nakajima T, Hamada E, Flecainide inhibits the transient outward current in atrial myocytes isolated from the rabbit heart. J Pharmacol Exp Ther. 1995 Jul;274(1):315-21.  [Content Brief]

    [2]. Desaphy JF, De Luca A, Didonna MP, Different flecainide sensitivity of hNav1.4 channels and myotonic mutants explained by state-dependent block. J Physiol. 2004 Jan 15;554(Pt 2):321-34.  [Content Brief]

    [3]. Kohli V. Oral flecainide is effective in management of refractory tachycardia in infants. Indian Heart J. 2013 Mar-Apr;65(2):168-71.  [Content Brief]

  • [1]. Yamashita T, Nakajima T, Hamada E, Flecainide inhibits the transient outward current in atrial myocytes isolated from the rabbit heart. J Pharmacol Exp Ther. 1995 Jul;274(1):315-21.

    [2]. Desaphy JF, De Luca A, Didonna MP, Different flecainide sensitivity of hNav1.4 channels and myotonic mutants explained by state-dependent block. J Physiol. 2004 Jan 15;554(Pt 2):321-34.

    [3]. Kohli V. Oral flecainide is effective in management of refractory tachycardia in infants. Indian Heart J. 2013 Mar-Apr;65(2):168-71.

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 2.1080 mL 10.5399 mL 21.0797 mL 52.6993 mL
5 mM 0.4216 mL 2.1080 mL 4.2159 mL 10.5399 mL
10 mM 0.2108 mL 1.0540 mL 2.1080 mL 5.2699 mL
15 mM 0.1405 mL 0.7027 mL 1.4053 mL 3.5133 mL
20 mM 0.1054 mL 0.5270 mL 1.0540 mL 2.6350 mL
25 mM 0.0843 mL 0.4216 mL 0.8432 mL 2.1080 mL
30 mM 0.0703 mL 0.3513 mL 0.7027 mL 1.7566 mL
40 mM 0.0527 mL 0.2635 mL 0.5270 mL 1.3175 mL
DMSO 50 mM 0.0422 mL 0.2108 mL 0.4216 mL 1.0540 mL
60 mM 0.0351 mL 0.1757 mL 0.3513 mL 0.8783 mL
80 mM 0.0263 mL 0.1317 mL 0.2635 mL 0.6587 mL
100 mM 0.0211 mL 0.1054 mL 0.2108 mL 0.5270 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Flecainide acetate Related Classifications

  • Membrane Transporter/Ion Channel
  • Sodium Channel
Help & FAQs

Keywords:

Flecainide54143-56-5R-818R818R 818Sodium ChannelNa channelsNa+ channelsInhibitorinhibitorinhibit

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