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    Dronedarone HCl (SR33589)
    Dronedarone HCl (SR33589)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1670
    CAS #: 141625-93-6 Purity ≥98%

    Description: Dronedarone (slao known as SR33589) HCl is a non-iodinated amiodarone analogue which has been used as an effective and promising treatment for Atrial fibrillation (AF). Dronedarone works as a multichannel blocker targeting potassium channel, sodium channel and calcium channel. In vitro, dronedarone has been demonstrated to inhibit muscarinic acetylcholine receptor-operated K+ current IK(ACh) induced by carbachol or GTP-gamma-S with IC50 values of 10nm and<100nm, respectively, in cells isolated from guinea pig atria. 

    References: J Cardiovasc Pharmacol. 2000;36(6):802-5; Br J Pharmacol. 2001;133(5):625-34.

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    Molecular Weight (MW)593.22 
    FormulaC31H44N2O5S.HCl 
    CAS No.141625-93-6 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 80 mg/mL (134.9 mM)
    Water: <1 mg/mL
    Ethanol: 40 mg/mL (67.4 mM) 
    Other info

    Chemical Name: N-[2-butyl-3-[4-[3-(dibutylamino)propoxy]benzoyl]-1-benzofuran-5-yl]methanesulfonamide;hydrochloride

    InChi Key: DWKVCQXJYURSIQ-UHFFFAOYSA-N

    InChi Code: InChI=1S/C31H44N2O5S.ClH/c1-5-8-12-29-30(27-23-25(32-39(4,35)36)15-18-28(27)38-29)31(34)24-13-16-26(17-14-24)37-22-11-21-33(19-9-6-2)20-10-7-3;/h13-18,23,32H,5-12,19-22H2,1-4H3;1H

    SMILES Code: CCCCC1=C(C2=C(O1)C=CC(=C2)NS(=O)(=O)C)C(=O)C3=CC=C(C=C3)OCCCN(CCCC)CCCC.Cl           

    SynonymsSR-33589; SR 33589; SR33589; Dronedarone Hydrochloride; 4CH-007232; D4689; W3083; D03914; S-7529; MCULE-2160502046; RL01735; RTC-070901; AK-72887; BC201083; BR-72887; HY-75839; KB-76727; AB2000517; ST2413542; Dronedarone HCl; UNII-FA36DV299Q


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    In Vitro

    In vitro activity: 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 VivoDronedarone 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. 
    Animal modelRats
    Formulation & Dosage
    References

    Br J Pharmacol. 2001 Jul;133(5):625-34; Br J Pharmacol. 2001 Jul;133(5):625-34; J Pharmacol Exp Ther. 2000 Jan;292(1):415-24. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

     

    Dronedarone HCl

    Effect of dronedarone on IK(ACh) elicited by ACh (10 μM). (a) ACh-induced current recorded in three cells before and after 3 min exposure. Br J Pharmacol. 2000 Jul;130(6):1315-20.
     

    Dronedarone HCl

    Dronedarone reduces IK(ACh) single channel activity by decreasing the open probability (Po). Br J Pharmacol. 2000 Jul;130(6):1315-20.
     

    Dronedarone HCl

    Concentration dependence of dronedarone-induced IK(ACh) block. Br J Pharmacol. 2000 Jul;130(6):1315-20.


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