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Dronedarone (formerly SR-33589; D-03914; S-7529; D-4689; W-3083; RL-01735; Multaq) is a non-iodinated amiodarone analog and a Class III antiarrhythmic as well as multi channel blocker approved for the treatment for Atrial fibrillation (AF).
| ln Vitro |
Drone successfully inhibited peak sodium currents in patch-clamp studies with human atrial myocytes, attaining 97% blockage at 3 μM [1]. Drone suppresses the delayed rectifier potassium current in guinea pig ventricular myocytes: the inward rectifier potassium current (IC50>30 μM), the slowly activated delayed rectifier potassium current (IC50=10 μM), and the fast activated delayed rectifier potassium current (IC50<3 μM). L-type calcium current (IC50=0.18 μM) [1] as well. In rabbit atrial node cells (IC50=63 nM) and guinea pig atrial cells (IC50=10 nM), dronedarone demonstrates potent inhibitory effects on acetylcholine-activated potassium current (IK-Ach). IK-Ach blockade by dronedarone is 100 times more effective than that of amiodarone [1]. Dronedarone binds non-competitively to β-adrenergic receptors (IC50=1.8 μM) to produce its anti-adrenergic effect by preventing the rise in adenylyl cyclase activity that an agonist causes [1]. In isolated guinea pig hearts, dose-dependent reduction in coronary perfusion pressure is induced by dose-daronedarone (0.01-1 μM). Its calcium current blockage may be connected to this action, which is not dependent on the nitric oxide synthase pathway [1].
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| ln Vivo |
Dronedarone (intraperitoneal injection; 25-100 mg/kg) shows dose-dependent anticonvulsant effects and raises the mouse electroconvulsive threshold [2].
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| Animal Protocol |
Animal/Disease Models: Tonic-clonic seizures in male albino Swiss outbred mice [2]
Doses: 25 mg/kg; 50 mg/kg; 75 mg/kg; 100 mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results: Shown Produces significant anticonvulsant effects. |
| References |
[1]. Chinmay Patel, et al. Dronedarone. Circulation. 2009 Aug 18;120(7):636-44.
[2]. Katarzyna M Sawicka, et al. Influence of dronedarone (a class III antiarrhythmic drug) on the anticonvulsant potency of four classical antiepileptic drugs in the tonic-clonic seizure model in mice. J Neural Transm (Vienna). 2019 Feb;126(2):115-122. |
| Molecular Formula |
C31H44N2O5S
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|---|---|
| Molecular Weight |
556.76
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| Exact Mass |
556.2971
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| CAS # |
141626-36-0
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| Related CAS # |
Dronedarone Hydrochloride;141625-93-6;Dronedarone-d6 hydrochloride;1329809-23-5
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| SMILES |
CCCCC1=C(C2=C(C=CC(NS(C)(=O)=O)=C2)O1)C(C3=CC=C(C=C3)OCCCN(CCCC)CCCC)=O
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| Synonyms |
SR 33589 SR33589D03914 S7529D4689 W3083 RL01735D-03914 S-7529D-4689 W-3083 RL-01735Multaq
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~89.81 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.49 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 (4.49 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), suspension 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 (4.49 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution. |
| Preparing Stock Solutions | 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 |
*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.
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