113558-89-7 Usage
Uses
Used in Pharmaceutical Research:
E-4031 is used as a research compound for studying the effects of hERG potassium channel inhibition. Its application in this field aids in understanding the underlying mechanisms of certain cardiac conditions and the development of potential therapeutic agents.
Used in Cardiology:
In the field of cardiology, E-4031 is used as a diagnostic tool to assess the impact of hERG channel blockers on the heart's electrical activity. This helps in identifying potential antiarrhythmic drugs and understanding their effects on cardiac function.
Used in Drug Development:
E-4031 is employed as a reference compound in the development of new drugs targeting the hERG potassium channel. Its use in this context is crucial for evaluating the safety and efficacy of novel compounds in preclinical and clinical trials.
Used in Safety Pharmacology:
E-4031 is utilized as a tool in safety pharmacology to predict the potential cardiotoxic effects of new drug candidates. By assessing the interaction of these candidates with the hERG channel, researchers can minimize the risk of developing drugs that may cause adverse cardiac events.
in vitro
it has been reported that e-4031 could induce eads or tdp, and such induction correlated with a significant increase in variability of repolarization. in addition, e-4031 at 0.1 um was able to significantly prolong cycle length, action potential duration, and depolarized maximum diastolic potential. e-4031could also reduce the upstroke velocity of the action potential as well as the diastolic depolarization rate [1].
in vivo
animal study showed that e-4031 at 0.01 and 0.1 mg/kg could provide effective in-vitro plasma concentrations to significantly inhibit ikr and thus delayed the repolarization beyond the initiation of diastole, leading to the inversion of electro-mechanical coupling, which provides an ideal proarrhythmic substrate [2]. another sutdy found that e-4031 could prolong qt interval and ari in all lv layers, though the magnitude of prolongation was greatest in mid, particularly during bradycardia [3].
IC 50
7.7 nm for herg
References
1) Ficker et al. (2002), The binding site for channel blockers that rescue misprocessed human long QT syndrome type 2 ether-a-gogo gene (HERG) mutations; J. Biol. Chem., 277 4989
2) Wettwer et al. (1991), Effects of the new class III antiarrhythmic drug E-4031 on myocardial contractility and electrophysical parameters; J. Cardiovasc. Pharmacol., 17 480
Check Digit Verification of cas no
The CAS Registry Mumber 113558-89-7 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,1,3,5,5 and 8 respectively; the second part has 2 digits, 8 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 113558-89:
(8*1)+(7*1)+(6*3)+(5*5)+(4*5)+(3*8)+(2*8)+(1*9)=127
127 % 10 = 7
So 113558-89-7 is a valid CAS Registry Number.
InChI:InChI=1/C21H27N3O3S/c1-16-4-3-5-19(22-16)12-15-24-13-10-18(11-14-24)21(25)17-6-8-20(9-7-17)23-28(2,26)27/h3-9,18,23H,10-15H2,1-2H3
113558-89-7Relevant articles and documents
Piperidine derivative and pharmaceutical composition containing the same
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, (2008/06/13)
A new piperidine compound is pharmacologically effective for treatment of the arrythmia and is defined by the formula: STR1 in which R1 is a lower alkyl or a tolyl, R2 is hydrogen, hydroxyl, a lower alkoxy or a lower alkyl, R3 is hydrogen, a lower alkyl,
