Dronedarone HCl
Catalog No.S2114 Synonyms: SR33589
Molecular Weight(MW): 593.22
Dronedarone HCl is a multichannel blocker targeting potassium channel, sodium channel and calcium channel, used as an antiarrhythmic drug for treatment of atrial fibrillation (AF).
Purity & Quality Control
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Biological Activity
| Description | Dronedarone HCl 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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| Targets |
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| 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] |
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| 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] |
Protocol
Solubility (25°C)
| In vitro | DMSO | 80 mg/mL (134.85 mM) |
|---|---|---|
| Ethanol | 40 mg/mL (67.42 mM) | |
| Water | Insoluble |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 593.22 |
|---|---|
| Formula | C31H44N2O5S.HCl |
| CAS No. | 141625-93-6 |
| Storage | powder |
| Synonyms | SR33589 |
Bio Calculators
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Clinical Trial Information
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT01522651 | Completed | Atrial Fibrillation | Gilead Sciences | January 2012 | Phase 2 |
| NCT01430806 | Unknown status | ICD|ICD SHOCKS|DRONEDARONE | Rabin Medical Center | October 2011 | -- |
| NCT01991119 | Completed | Atrial Fibrillation | Samsung Medical Center | May 2011 | -- |
| NCT01266681 | Unknown status | Atrial Fibrillation | Eastbourne General Hospital | March 2011 | -- |
| NCT01306162 | Completed | Healthy | Boehringer Ingelheim | February 2011 | Phase 1 |
| NCT01182376 | Completed | Atrial Fibrillation | University of Utah|Sanofi | November 2010 | Phase 3 |
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