Home Transmembrane Transporters Potassium Channel inhibitor - Sodium Channel inhibitor - Calcium Channel inhibitor Dronedarone HCl For research use only.

Dronedarone HCl

Synonyms: SR33589

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 HCl Chemical Structure

Dronedarone HCl Chemical Structure

CAS: 141625-93-6

Selleck's Dronedarone HCl has been cited by 4 Publications

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Purity & Quality Control

Batch: S211401 DMSO] 80 mg/mL] false] Ethanol] 40 mg/mL] false] Water] Insoluble] false Purity: 99.98%
99.98

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Biological Activity

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).
Targets
Potassium channel [1] Sodium channel [1] Calcium channel [1]
In vitro
In vitro 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. [1] 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. [2] 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. [3]
In Vivo
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. [4]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01430806 Unknown status ICD|ICD SHOCKS|DRONEDARONE Rabin Medical Center October 2011 Not Applicable
NCT01266681 Unknown status Atrial Fibrillation Eastbourne General Hospital March 2011 Not Applicable
NCT01199081 Completed Atrial Fibrillation Sanofi October 2010 Phase 4
NCT01213368 Completed Atrial Fibrillation Sanofi September 2010 Phase 2
NCT01140581 Completed Atrial Fibrillation Sanofi September 2010 Phase 4
NCT01070667 Unknown status Paroxysmal Atrial Fibrillation Eastbourne General Hospital March 2010 Phase 4

Chemical lnformation & Solubility

Molecular Weight 593.22 Formula

C31H44N2O5S.HCl
CAS No. 141625-93-6 SDF Download Dronedarone HCl SDF
Smiles CCCCC1=C(C2=C(O1)C=CC(=C2)NS(=O)(=O)C)C(=O)C3=CC=C(C=C3)OCCCN(CCCC)CCCC.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 80 mg/mL ( (134.85 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 40 mg/mL

Water : Insoluble


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