N-Desbutyl Dronedarone (hydrochloride)

  CAY-34888-25 25 mg

Data Sheet:     SDS:    

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197431-02-0  

A solid  

≥95%  

537,1  

-20  

-20  

1460  

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Description

 

N-Desbutyl dronedarone is an active metabolite of the antiarrhythmic agent dronedarone (Item No. 9000543).{58755,58756,58757} It is formed from dronedarone by cytochrome P450s (CYPs) and monoamine oxidase (MAO) in human hepatocyte preparations.{58758} N-Desbutyl dronedarone inhibits the binding of 3,3',5-triiodo-L-thyronine (T3; Item No. 16028) to the thyroid hormone receptors TRα1 and TRβ1 (IC50s = 59 and 280 µM for the chicken and human receptors, respectively).{58755} It inhibits CYP2J2-mediated formation of 14,15-EET from arachidonic acid and soluble epoxide hydrolase-mediated formation of 14,15-DHET from 14,15-EET (IC50s = 1.59 and 2.73 µM, respectively, in cell-free assays).{58756} N-Desbutyl dronedarone decreases intracellular ATP levels in H9c2 rat cardiomyocytes (IC50 = 1.07 µM) and inhibits mitochondrial complex I, also known as NADH dehydrogenase, and mitochondrial complex II, also known as succinate dehydrogenase, activities in isolated rat heart mitochondria (IC50s = 11.94 and 24.54 µM, respectively).{58757}

 

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