| Size | Price | Stock | Qty |
|---|---|---|---|
| 1g |
|
||
| 2g |
|
||
| 5g |
|
||
| 10g |
|
||
| Other Sizes |
Purity: ≥98%
Propafenone HCl (formerly SA-79; SA79; Rytmonorm; Pronon; Arythmol; Baxarytmon; Cuxafenon; Fenoprain), the hydrochloride salt of Propafenone, is an approved class 1C anti-arrhythmic drug. It acts as a sodium channel protein inhibitor, which has been used to treat illnesses associated with rapid heart beats such as atrial and ventricular arrhythmias.
| Targets |
Voltage-gated sodium channels[1]
- Rapidly activating delayed rectifier K+ current (IKr)[1] - L-type calcium channels [1] |
|---|---|
| ln Vitro |
In isolated cardiac myocytes (human, canine, rabbit), Propafenone HCl (SA-79) potently blocks voltage-gated sodium channels in a use- and voltage-dependent manner. It suppresses the fast inward sodium current (INa), reducing the maximum rate of depolarization (Vmax) of cardiac action potentials. At therapeutic concentrations (0.5-2 μM), it prolongs the action potential duration (APD) by weakly blocking IKr and L-type calcium channels. Additionally, the drug inhibits abnormal automaticity and reentrant conduction in hyperexcitable cardiac cells[1]
|
| ln Vivo |
A traditional antiarrhythmic medication called propafenone (SA-79) hydrochloride is used to treat diseases like atrial and ventricular arrhythmias, which are characterized by fast heartbeats. Based on a revised classification system for rhinitis, the Allergic Rhinitis Affecting (ARIA) management guidelines prescribe intranasal antihistamines for the first-line care of intermittent intermittent, moderate/severe intermittent, and intermittent persistent rhinitis. Reduced cell excitability is the outcome of propafenone hydrochloride's disruption of sodium ion influx into cardiomyocytes. In comparison to Class Ia or Ib, propafenone hydrochloride is more selective for cells and has a higher rate, but it also blocks normal cells more thoroughly. Propafenone hydrochloride's additional action as a beta-preteraergic blocker, which results in bradycardia and arrest spasm, makes it an obvious classic Class Ic antiarrhythmic medication [1].
In canine models of experimentally induced atrial fibrillation (AF) and ventricular tachycardia (VT), intravenous administration of Propafenone HCl (SA-79) (1-2 mg/kg) converts AF to sinus rhythm in 60-80% of cases and suppresses VT episodes. Oral administration (10-20 mg/kg, twice daily) maintains sinus rhythm and reduces the frequency of recurrent arrhythmias. In rabbit models of atrioventricular nodal reentrant tachycardia (AVNRT), the drug prolongs the effective refractory period of the atrioventricular node, terminating reentrant circuits[1] |
| Cell Assay |
Cardiac myocyte electrophysiology assay: Cardiac myocytes were isolated from adult hearts via enzymatic dissociation and plated on glass coverslips. Propafenone HCl (SA-79) was added to the extracellular recording solution at concentrations of 0.1-5 μM. Whole-cell patch-clamp recordings were performed to measure INa, IKr, and L-type calcium current (ICa,L). Voltage protocols included depolarizing steps to activate specific currents, and peak current amplitudes and kinetics were analyzed to evaluate blocking effects[1]
- Action potential recording assay: Isolated cardiac myocytes were superfused with physiological saline containing Propafenone HCl (SA-79) (0.5-2 μM). Action potentials were recorded using intracellular microelectrodes or patch-clamp techniques, and parameters such as Vmax, APD50, and APD90 were quantified[1] |
| Animal Protocol |
Atrial fibrillation/ventricular tachycardia dog model: Adult mongrel dogs (15-25 kg) were anesthetized, and electrodes were implanted to induce AF/VT via electrical stimulation. Propafenone HCl (SA-79) was administered intravenously as a bolus (1-2 mg/kg) followed by a continuous infusion (0.05-0.1 mg/kg/min) if needed. Cardiac rhythm was monitored via electrocardiography for 2 hours to assess arrhythmia conversion[1]
- Oral maintenance animal model: Rats (200-250 g) were administered Propafenone HCl (SA-79) dissolved in drinking water or as a gavage formulation (10-20 mg/kg, twice daily) for 2 weeks. Arrhythmias were induced weekly via electrical stimulation, and the drug's efficacy in suppressing arrhythmias was evaluated by comparing pre- and post-treatment arrhythmia incidence[1] |
| ADME/Pharmacokinetics |
Absorption: Propamidrone hydrochloride (SA-79) is rapidly and almost completely absorbed orally (95%), but its oral bioavailability is low (3-40%) due to extensive first-pass metabolism in the liver [1]. Distribution: The drug has a large volume of distribution (2-3 L/kg) and is widely distributed in the heart, liver, and lungs [1]. Metabolism: It is mainly metabolized in the liver by cytochrome P450 2D6 (CYP2D6), with less contribution from CYP1A2 and CYP3A4. Plasma concentrations are significantly higher in those with poor metabolic capacity (CYP2D6 polymorphism) [1]. Excretion: Approximately 10% of the original drug and 90% of the metabolites are excreted in the urine; a small amount of the drug is excreted in the feces [1]. Half-life: The elimination half-life is 2 to 10 hours, and the half-life is longer (up to 17 hours) in those with slower metabolism [1].
|
| Toxicity/Toxicokinetics |
Plasma protein binding: Propapane hydrochloride (SA-79) is highly bound to plasma proteins (95-97%), primarily albumin [1] - Cardiovascular toxicity: High doses or overdose may cause QT interval prolongation, torsades de pointes (TdP), bradycardia, and hypotension. Patients with heart failure or electrolyte disturbances are at increased risk [1] - Non-cardiovascular toxicity: Common side effects include gastrointestinal symptoms (nausea, vomiting, constipation), central nervous system reactions (dizziness, blurred vision, tremor), and rash (rare) [1] - Hepatotoxicity/nephrotoxicity: Rare cases of hepatocellular damage or renal impairment have been reported, which are usually reversible upon discontinuation [1] - Drug interactions: Concomitant use with β-adrenergic blockers, digoxin, or other antiarrhythmic drugs increases the risk of bradycardia and hypotension. CYP2D6 inhibitors (such as fluoxetine and paroxetine) increase the concentration of propafenone in plasma [1]
|
| References | |
| Additional Infomation |
Propafenone hydrochloride is the monohydrochloride salt of propafenone. It is a class 1C antiarrhythmic drug with local anesthetic activity, used to treat supraventricular and ventricular arrhythmias. It is an antiarrhythmic drug containing propafenone (1+). Propafenone hydrochloride is the hydrochloride form of propafenone with class 1C antiarrhythmic activity. Propafenone hydrochloride stabilizes neuronal membranes by binding to and inhibiting the activity of voltage-gated sodium channels, thereby reducing sodium ion influx required for impulse initiation and conduction in Purkinje cells and cardiomyocytes. This drug significantly inhibits phase 0 conduction in the atrioventricular node and His-Purkinje tissue, prolonging the effective refractory period, thereby significantly reducing excitability, conduction velocity, and automaticity, thus counteracting atrial and ventricular arrhythmias. A particularly effective antiarrhythmic drug for ventricular arrhythmias. It also has weak β-receptor blocking activity. See also: propafenone (containing the active moiety).
Propafenone hydrochloride (SA-79) is a class IC antiarrhythmic drug with potent sodium channel blocking activity[1] - Clinical indications include the treatment of life-threatening ventricular arrhythmias, conversion of atrial fibrillation/flutter to sinus rhythm, and prevention of recurrent paroxysmal supraventricular tachycardia[1] - Its antiarrhythmic mechanism includes slowing cardiac conduction (through sodium channel blockade) and prolonging the refractory period, thereby terminating reentrant arrhythmias and inhibiting abnormal automaticity[1] - The drug is available in oral (tablets, extended-release capsules) and intravenous formulations for the treatment of acute and chronic arrhythmias[1] - It has been approved by the FDA for use in adults only; its use in pediatric patients is off-label and requires careful dose adjustment[1] |
| Molecular Formula |
C21H27NO3.HCL
|
|
|---|---|---|
| Molecular Weight |
377.9
|
|
| Exact Mass |
377.175
|
|
| CAS # |
34183-22-7
|
|
| Related CAS # |
(S)-Propafenone;107381-32-8;Propafenone;54063-53-5;Propafenone-d7 hydrochloride;1219799-06-0;Propafenone-d5 hydrochloride;1346605-05-7;Propafenone-d5 Ethyl hydrochloride;1398066-02-8;Propafenone-(phenyl-dd5) (hydrochloride);93909-48-9
|
|
| PubChem CID |
36708
|
|
| Appearance |
White to off-white solid powder
|
|
| Boiling Point |
519.6ºC at 760 mmHg
|
|
| Melting Point |
165-1670C
|
|
| Flash Point |
268ºC
|
|
| LogP |
4.434
|
|
| Hydrogen Bond Donor Count |
3
|
|
| Hydrogen Bond Acceptor Count |
4
|
|
| Rotatable Bond Count |
11
|
|
| Heavy Atom Count |
26
|
|
| Complexity |
368
|
|
| Defined Atom Stereocenter Count |
0
|
|
| SMILES |
CCCNCC(COC1=CC=CC=C1C(=O)CCC2=CC=CC=C2)O.Cl
|
|
| InChi Key |
XWIHRGFIPXWGEF-UHFFFAOYSA-N
|
|
| InChi Code |
InChI=1S/C21H27NO3.ClH/c1-2-14-22-15-18(23)16-25-21-11-7-6-10-19(21)20(24)13-12-17-8-4-3-5-9-17;/h3-11,18,22-23H,2,12-16H2,1H3;1H
|
|
| Chemical Name |
1-[2-[2-hydroxy-3-(propylamino)propoxy]phenyl]-3-phenylpropan-1-one;hydrochloride
|
|
| Synonyms |
|
|
| HS Tariff Code |
2934.99.9001
|
|
| 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)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.62 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 (6.62 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 (6.62 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 | 2.6462 mL | 13.2310 mL | 26.4620 mL | |
| 5 mM | 0.5292 mL | 2.6462 mL | 5.2924 mL | |
| 10 mM | 0.2646 mL | 1.3231 mL | 2.6462 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA