1. GPCR/G Protein
    Neuronal Signaling
    Membrane Transporter/Ion Channel
    Metabolic Enzyme/Protease
    Autophagy
  2. mAChR
    Sodium Channel
    Calcium Channel
    Adrenergic Receptor
    Cytochrome P450
    Autophagy
  3. Dronedarone

Dronedarone (Synonyms: SR 33589)

Cat. No.: HY-A0016 Purity: 99.63%
Handling Instructions

Dronedarone (SR 33589), a derivative of amiodarone (HY-14187), is a class III antiarrhythmic agent for the study of atrial fibrillation (AF) and atrial flutter. Dronedarone is a potent blocker of multiple ion currents, including potassium current, sodium current, and L-type calcium current, and exhibits antiadrenergic effects by noncompetitive binding to β-adrenergic receptors. Dronedarone is a substrate for and a moderate inhibitor of CYP3A4.

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

Dronedarone Chemical Structure

Dronedarone Chemical Structure

CAS No. : 141626-36-0

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10 mM * 1 mL in DMSO USD 66 In-stock
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Description

Dronedarone (SR 33589), a derivative of amiodarone (HY-14187), is a class III antiarrhythmic agent for the study of atrial fibrillation (AF) and atrial flutter. Dronedarone is a potent blocker of multiple ion currents, including potassium current, sodium current, and L-type calcium current, and exhibits antiadrenergic effects by noncompetitive binding to β-adrenergic receptors. Dronedarone is a substrate for and a moderate inhibitor of CYP3A4[1].

In Vitro

In patch clamp experiments using human atrial myocytes, Dronedarone produces potent blockade of peak sodium current, resulting in a 97% block at 3 μM[1].
In guinea pig ventricular myocytes, Dronedarone inhibits the rapidly activating delayed-rectifier potassium current (IC50<3 μM), the slowly activating delayed-rectifier potassium current (IC50=10 μM), the inward rectifier potassium current (IC50>30 μM), and L-type calcium current (IC50=0.18 μM)[1].
Dronedarone exhibits strong inhibitory effects on the acetylcholine-activated potassium current (IK-Ach) in rabbit inoatrial nodal cells (IC50=63 nM) and guinea pig atrial cells (IC50=10 nM). Blockade of IK-Ach by dronedarone is 100 times more potent than that of amiodarone[1].
Dronedarone exerts its antiadrenergic effects by noncompetitive binding to β-adrenergic receptors (IC50=1.8 μM) and inhibition of agonist-induced increases in adenylate cyclase activity[1].
Dronedarone (0.01-1 μM) induces a concentration-dependent reduction of coronary perfusion pressure in isolated guinea pig hearts, effects that are independent of the nitric oxide synthase pathway and possibly related to its calcium current blockade[1].

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

In Vivo

Dronedarone (intraperitoneal injection; 25-100 mg/kg) exhibits anticonvulsant effects in a dose-dependent manner and increases the threshold for electroconvulsions in mice[2].

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

Animal Model: Tonic-clonic seizures in male albino Swiss outbred mice[2]
Dosage: 25 mg/kg; 50 mg/kg; 75 mg/kg; 100 mg/kg
Administration: Intraperitoneal injection
Result: Showed significant anticonvulsant effects.
Clinical Trial
Molecular Weight

556.76

Formula

C₃₁H₄₄N₂O₅S

CAS No.

141626-36-0

SMILES

CCCCC1=C(C2=C(C=CC(NS(C)(=O)=O)=C2)O1)C(C3=CC=C(C=C3)OCCCN(CCCC)CCCC)=O

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 : ≥ 100 mg/mL (179.61 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7961 mL 8.9805 mL 17.9611 mL
5 mM 0.3592 mL 1.7961 mL 3.5922 mL
10 mM 0.1796 mL 0.8981 mL 1.7961 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: ≥ 3 mg/mL (5.39 mM); Clear solution

  • 2.

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

    Solubility: ≥ 3 mg/mL (5.39 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.63%

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Keywords:

DronedaroneSR 33589SR33589SR-33589mAChRSodium ChannelCalcium ChannelAdrenergic ReceptorCytochrome P450AutophagyMuscarinic acetylcholine receptorNa channelsNa+ channelsCa2+ channelsCa channelsBeta ReceptorCYPsatrial myocyteAFpotassium currentantiadrenergicinoatrial nodalcoronary perfusionatrial flutterInhibitorinhibitorinhibit

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