For research use only.
Catalog No.S2114 Synonyms: SR33589
CAS No. 141625-93-6
Dronedarone HCl (SR33589) is a multichannel blocker targeting potassium channel, sodium channel and calcium channel, used as an antiarrhythmic drug for treatment of atrial fibrillation (AF).
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Results of hit validation experiments for these four compounds for animals treated at L1 stage at four different concentrations (0.5, 5, 25, and 50 μM). The blue bars represent the values obtained from the original screen as reference points. Error bars are standard error of the mean. Statistical significance for all different doses for individual compounds was calculated with respect to the lowest concentration using two-tailed, t-test (nZ70 animals except n = 37 for Geld 25 μM). The statistical significance values are represented as P<0.05 (*) and P<0.005 (**).
Nat Commun. 2016, 7:13023. Dronedarone HCl purchased from Selleck.
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Choose Selective Potassium Channel Inhibitors
|Description||Dronedarone HCl (SR33589) is a multichannel blocker targeting potassium channel, sodium channel and calcium channel, used as an antiarrhythmic drug for treatment of atrial fibrillation (AF).|
Dronedarone reduces the incidence of early and delayed after depolarizations evoked by 1 mM Dofetilide and 0.2 mM Strophantidine in Purkinje fibres. Dronedarone (10 mM) markedly reduces the L-type calcium current (76.5%) and the rapid component of the delayed rectifier potassium current (97%) in ventricular myocytes.  Dronedarone inhibits the activity of I(K(ACh)) channels recorded from cell-attached patches by reducing the channel open probability (from 0.56 to 0.11) without modification of the single-channel conductance in single cells isolated from sinoatrial node (SAN) tissue of rabbit hearts.  Dronedarone exhibits a state-dependent inhibition of the fast Na(+) channel current with an IC50 of 0.7 μM in guinea pig ventricular myocytes, when the holding potential (V (hold)) is -80 mV. Dronedarone blocks Ca(2+) currents elicited by rectangular pulses at V (hold) = -40 mV with IC50 value of 0.4 μM, whereas at V (hold) = -80 mV, Dronedarone (10 μM) blocks only 20 % of the current. 
|In vivo||Dronedarone increases action potential duration in normal hearts of rats. Dronedarone reduces the late sustained K(+) current, I(K) (or Isus) by 69%. Dronedarone induces only a tonic block of I(K). Dronedarone induces a weak increase in the fast transient outward current, I(to), in rats after myocardial infarction. |
|In vitro||DMSO||80 mg/mL (134.85 mM)|
|Ethanol||40 mg/mL (67.42 mM)|
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|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
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|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01430806||Unknown status||Drug: Dronedarone arm|Drug: Dronedarone||ICD|ICD SHOCKS|DRONEDARONE||Rabin Medical Center||October 2011||Not Applicable|
|NCT01266681||Unknown status||Drug: amiodarone|Drug: Dronedarone||Atrial Fibrillation||Eastbourne General Hospital||March 2011||Not Applicable|
|NCT01199081||Completed||Drug: Dronedarone||Atrial Fibrillation||Sanofi||October 2010||Phase 4|
|NCT01213368||Completed||Drug: DRONEDARONE (SR33589)|Drug: placebo||Atrial Fibrillation||Sanofi||September 2010||Phase 2|
|NCT01140581||Completed||Drug: DRONEDARONE||Atrial Fibrillation||Sanofi||September 2010||Phase 4|
|NCT01070667||Unknown status||Drug: Dronedarone|Drug: Placebo||Paroxysmal Atrial Fibrillation||Eastbourne General Hospital||March 2010||Phase 4|
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