1. Membrane Transporter/Ion Channel
  2. Sodium Channel
  3. Flecainide acetate

Flecainide acetate (Synonyms: R-818)

Cat. No.: HY-17429 Purity: 99.87%
Handling Instructions

Flecainide acetate (R-818) is a class 1C antiarrhythmic drug 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.

For research use only. We do not sell to patients.

Flecainide acetate Chemical Structure

Flecainide acetate Chemical Structure

CAS No. : 54143-56-5

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Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 66 In-stock
Estimated Time of Arrival: December 31
Solid
10 mg USD 60 In-stock
Estimated Time of Arrival: December 31
50 mg USD 168 In-stock
Estimated Time of Arrival: December 31
100 mg USD 228 In-stock
Estimated Time of Arrival: December 31
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Description

Flecainide acetate (R-818) is a class 1C antiarrhythmic drug 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].

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

Clinical Trial
Molecular Weight

474.39

Formula

C₁₉H₂₄F₆N₂O₅

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (105.40 mM; Need ultrasonic)

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
10 mM 0.2108 mL 1.0540 mL 2.1080 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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Product Name:
Flecainide acetate
Cat. No.:
HY-17429
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