Dofetilide

Dofetilide Structure
Dofetilide structure
Common Name Dofetilide
CAS Number 115256-11-6 Molecular Weight 441.565
Density 1.3±0.1 g/cm3 Boiling Point 614.1±65.0 °C at 760 mmHg
Molecular Formula C19H27N3O5S2 Melting Point 147-1490C
MSDS Chinese USA Flash Point 325.2±34.3 °C
Symbol GHS07 GHS08
GHS07, GHS08
Signal Word Danger

Synchronous systolic subcellular Ca2+-elevations underlie ventricular arrhythmia in drug-induced long QT type 2.

Circ. Arrhythm. Electrophysiol. 8 , 703-12, (2015)

Repolarization delay is a common clinical problem, which can promote ventricular arrhythmias. In myocytes, abnormal sarcoplasmic reticulum Ca(2+)-release is proposed as the mechanism that causes early afterdepolarizations, the cellular equivalent of ectopic-a...

The Link between Inactivation and High-Affinity Block of hERG1 Channels.

Mol. Pharmacol. 87 , 1042-50, (2015)

Block of human ether-à-go-go-related gene 1 (hERG1) K(+) channels by many drugs delays cardiac repolarization, prolongs QT interval, and is associated with an increased risk of cardiac arrhythmia. Preferential block of hERG1 channels in an inactivated state h...

Relevance of calmodulin/CaMKII activation for arrhythmogenesis in the AV block dog.

Heart Rhythm 9(11) , 1875-83, (2012)

The calcium-dependent signaling molecules calcineurin and calcium/calmodulin-dependent protein kinase II (CaMKII) both have been linked to decompensated hypertrophy and arrhythmias. CaMKII is also believed to be involved in acute modulation of ion channels.Th...

Characterization of A-935142, a hERG enhancer, in the presence and absence of standard hERG blockers.

Life Sci. 90(15-16) , 607-11, (2012)

In a previous study we found that A-935142 enhanced hERG current in a concentration-dependent manner by facilitating activation, reducing inactivation, and slowing deactivation (Su et al., 2009). A-935142 also shortened action potential duration (APD90) in ca...

Proarrhythmia Risk Assessment in Human Induced Pluripotent Stem Cell-Derived Cardiomyocytes Using the Maestro MEA Platform.

Toxicol. Sci. 147 , 286-95, (2015)

Evaluation of stem cell-derived cardiomyocytes (SC-CM) using multi-electrode array (MEA) has attracted attention as a novel model to detect drug-induced arrhythmia. An experiment was conducted to determine if MEA recording from human induced pluripotent SC-CM...

Inhibition of Schistosoma mansoni ether-a-go-go related gene-encoded potassium channels leads to hypermotility and impaired egg production.

Exp. Parasitol. 158 , 48-54, (2015)

The purpose of this work was to investigate the effect of ether-a-go-go related gene (ERG) potassium channel inhibition on Schistosoma mansoni. Use of dofetilide to block the schistosome ERGs resulted in a striking 'corkscrew' effect. The worms were unable to...

Mild Pd-catalyzed N-arylation of methanesulfonamide and related nucleophiles: avoiding potentially genotoxic reagents and byproducts.

Org. Lett. 13(10) , 2564-7, (2011)

A convenient, general, and high yielding Pd-catalyzed cross-coupling of methanesulfonamide with aryl bromides and chlorides is reported. The use of this method eliminates concern over genotoxic impurities that can arise when an aniline is reacted with methane...

Vacuolar ATPase driven potassium transport in highly metastatic breast cancer cells.

Biochim. Biophys. Acta 1832(10) , 1734-43, (2013)

Breast cancer is the second leading cause of death in women and thus has received a great deal of attention by researchers. Recent studies suggested decreased occurrence of cancer in patients treated with cardiac glycosides (CGs) for heart conditions. Because...

Dofetilide versus quinidine for atrial flutter: viva la difference!?

J. Cardiovasc. Electrophysiol. 7(9) , 828-32, (1996)

Dofetilide is more effective than quinidine to terminate atrial flutter in this animal model. It is also more capable of lengthening refractoriness more uniformly than quinidine. While the investigators describe local changes in refractoriness and dispersion ...

Repolarization reserve determines drug responses in human pluripotent stem cell derived cardiomyocytes.

Stem Cell Res. 10(1) , 48-56, (2013)

Unexpected induction of arrhythmias in the heart is still one of the major risks of new drugs despite recent improvements in cardiac safety assays. Here we address this in a novel emerging assay system. Eleven reference compounds were administrated to spontan...