2016年6月12日星期日

E-4031|cas 113559-13-0|DC Chemicals

E-4031|cas 113559-13-0|DC Chemicals

E-4031 is a benzenesulfonamide antiarrhythmic agent; blocks the ATP-sensitive potassium channel.

IC50 value:

Target: K+ channel blocker

in vitro: Dofetilide and E-4031 induced EADs or TdP in all assays (50-83%), and the induction correlated with a significant increase in beat-to-beat variability of repolarization .

Product Name: E-4031|Cat No: DC9595|Cas: 113559-13-0|Molecule Formular: C21H29Cl2N3O3S|Molecule Weight: 474.4443|Other names: E-4031

E-4031 is a benzenesulfonamide antiarrhythmic agent; blocks the ATP-sensitive potassium channel.
in vitro: Dofetilide and E-4031 induced EADs or TdP in all assays (50-83%), and the induction correlated with a significant increase in beat-to-beat variability of repolarization. E-4031 (0.1 mumol/L) significantly prolonged cycle length and action potential duration, depolarized maximum diastolic potential, and reduced both the upstroke velocity of the action potential and the diastolic depolarization rate.
in vivo: E-4031 in doses of 0.01 and 0.1 mg/kg that can provide the plasma concentrations effectively to inhibit IKrin vitro significantly delayed the repolarization beyond the initiation of diastole, resulting in the inversion of electro-mechanical coupling, which provides an ideal proarrhythmic substrate, while the durations of left ventricular systole and diastole remained the same. Bepridil and E-4031 prolonged QT interval and ARI in all LV layers, though the magnitude of prolongation was greatest in Mid, increasing the transmural ARI dispersion, particularly during bradycardia.

For research only, not for human use!

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