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113559-13-0,MFCD01754739
Catalog No.:AA0008W4

113559-13-0 | E-4031

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1mg
98%
in stock  
$18.00   $13.00
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5mg
98%
in stock  
$65.00   $46.00
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10mg
98%
in stock  
$110.00   $77.00
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25mg
98%
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$258.00   $181.00
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50mg
98%
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$428.00   $300.00
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  • Technical Information
  • Properties
  • Downstream Synthesis Route
  • Literature
  • Request for Quotation
  • Download SDS
  • Technical Information
  • Properties
  • Downstream Synthesis Route
  • Literature
Technical Information
Catalog Number:
AA0008W4
Chemical Name:
E-4031
CAS Number:
113559-13-0
Molecular Formula:
C21H29Cl2N3O3S
Molecular Weight:
474.4443
MDL Number:
MFCD01754739
SMILES:
Cc1cccc(n1)CCN1CCC(CC1)C(=O)c1ccc(cc1)NS(=O)(=O)C.Cl.Cl
Properties
Computed Properties
 
Complexity:
603  
Covalently-Bonded Unit Count:
3  
Heavy Atom Count:
30  
Hydrogen Bond Acceptor Count:
6  
Hydrogen Bond Donor Count:
3  
Rotatable Bond Count:
7  

Downstream Synthesis Route
Literature

Title: Aromatase knockout mice reveal an impact of estrogen on drug-induced alternation of murine electrocardiography parameters.

Journal: The Journal of toxicological sciences 20150601

Title: Investigation of a novel series of 2-hydroxyisoquinoline-1,3(2H,4H)-diones as human immunodeficiency virus type 1 integrase inhibitors.

Journal: Journal of medicinal chemistry 20140612

Title: Role of action potential configuration and the contribution of C²⁺a and K⁺ currents to isoprenaline-induced changes in canine ventricular cells.

Journal: British journal of pharmacology 20121001

Title: Functional characterization of ether-à-go-go-related gene potassium channels in midbrain dopamine neurons - implications for a role in depolarization block.

Journal: The European journal of neuroscience 20121001

Title: Cardiac tissue slices with prolonged survival for in vitro drug safety screening.

Journal: Journal of pharmacological and toxicological methods 20120901

Title: Transmural dispersion of repolarization as a preclinical marker of drug-induced proarrhythmia.

Journal: Journal of cardiovascular pharmacology 20120801

Title: Development of recombinant cell line co-expressing mutated Nav1.5, Kir2.1, and hERG for the safety assay of drug candidates.

Journal: Journal of biomolecular screening 20120701

Title: A novel method of selecting human embryonic stem cell-derived cardiomyocyte clusters for assessment of potential to influence QT interval.

Journal: Toxicology in vitro : an international journal published in association with BIBRA 20120301

Title: Inhibition of HERG1 K+ channel protein expression decreases cell proliferation of human small cell lung cancer cells.

Journal: Pflugers Archiv : European journal of physiology 20120201

Title: Understanding of molecular substructures that contribute to hERG K+ channel blockade: synthesis and biological evaluation of E-4031 analogues.

Journal: ChemMedChem 20120102

Title: Comparison of the IKr blockers moxifloxacin, dofetilide and E-4031 in five screening models of pro-arrhythmia reveals lack of specificity of isolated cardiomyocytes.

Journal: British journal of pharmacology 20120101

Title: Pharmacological blockade of IKs destabilizes spiral-wave reentry under β-adrenergic stimulation in favor of its early termination.

Journal: Journal of pharmacological sciences 20120101

Title: Dynamic link between histone H3 acetylation and an increase in the functional characteristics of human ESC/iPSC-derived cardiomyocytes.

Journal: PloS one 20120101

Title: hERG subunit composition determines differential drug sensitivity.

Journal: British journal of pharmacology 20110901

Title: Trafficking-deficient hERG K⁺ channels linked to long QT syndrome are regulated by a microtubule-dependent quality control compartment in the ER.

Journal: American journal of physiology. Cell physiology 20110701

Title: Late sodium current contributes to the reverse rate-dependent effect of IKr inhibition on ventricular repolarization.

Journal: Circulation 20110426

Title: Pyrimidine-2,4,6-trione derivatives and their inhibition of mutant SOD1-dependent protein aggregation. Toward a treatment for amyotrophic lateral sclerosis.

Journal: Journal of medicinal chemistry 20110414

Title: Chemotherapy resistance in acute lymphoblastic leukemia requires hERG1 channels and is overcome by hERG1 blockers.

Journal: Blood 20110120

Title: Trafficking defect and proteasomal degradation contribute to the phenotype of a novel KCNH2 long QT syndrome mutation.

Journal: PloS one 20110101

Title: Presence and functional role of the rapidly activating delayed rectifier K(+) current in left and right atria of adult mice.

Journal: European journal of pharmacology 20101215

Title: The subtype-specific effects of droperidol on action potential duration in cellular and computational models of long QT syndrome.

Journal: Anesthesia and analgesia 20100901

Title: Pharmacological activation of IKr impairs conduction in guinea pig hearts.

Journal: Journal of cardiovascular electrophysiology 20100801

Title: Effects of bepridil versus E-4031 on transmural ventricular repolarization and inducibility of ventricular tachyarrhythmias in the dog.

Journal: Pacing and clinical electrophysiology : PACE 20100801

Title: Characterization of the rapidly activating delayed rectifier potassium current, I (Kr), in HL-1 mouse atrial myocytes.

Journal: The Journal of membrane biology 20100601

Title: Pharmacological removal of human ether-à-go-go-related gene potassium channel inactivation by 3-nitro-N-(4-phenoxyphenyl) benzamide (ICA-105574).

Journal: Molecular pharmacology 20100101

Title: Acute effects of sex steroid hormones on susceptibility to cardiac arrhythmias: a simulation study.

Journal: PLoS computational biology 20100101

Title: Clobutinol delays ventricular repolarization in the guinea pig heart: comparison with cardiac effects of HERG K+ channel inhibitor E-4031.

Journal: Journal of cardiovascular pharmacology 20091201

Title: Erg K+ currents modulate excitability in mouse mitral/tufted neurons.

Journal: Pflugers Archiv : European journal of physiology 20091101

Title: Reduction of repolarization reserve unmasks the proarrhythmic role of endogenous late Na(+) current in the heart.

Journal: American journal of physiology. Heart and circulatory physiology 20090901

Title: Side chain flexibilities in the human ether-a-go-go related gene potassium channel (hERG) together with matched-pair binding studies suggest a new binding mode for channel blockers.

Journal: Journal of medicinal chemistry 20090723

Title: Ether-à-go-go-related gene K+ channels contribute to threshold excitability of mouse auditory brainstem neurons.

Journal: The Journal of physiology 20090601

Title: Docking model of drug binding to the human ether-à-go-go potassium channel guided by tandem dimer mutant patch-clamp data: a synergic approach.

Journal: Journal of medicinal chemistry 20090326

Title: The muscarinic inhibition of the potassium M-current modulates the action-potential discharge in the vestibular primary-afferent neurons of the rat.

Journal: Neuroscience 20090218

Title: The role of ether-a-go-go-related gene K(+) channels in glucocorticoid inhibition of adrenocorticotropin release by rat pituitary cells.

Journal: Regulatory peptides 20090108

Title: Acidosis inhibits spontaneous activity and membrane currents in myocytes isolated from the rabbit atrioventricular node.

Journal: Journal of molecular and cellular cardiology 20090101

Title: Ether-a-go-go-related gene 3 is the main candidate for the E-4031-sensitive potassium current in the pacemaker interstitial cells of Cajal.

Journal: American journal of physiology. Gastrointestinal and liver physiology 20081001

Title: Adrenaline reveals the torsadogenic effect of combined blockade of potassium channels in anaesthetized guinea pigs.

Journal: British journal of pharmacology 20080801

Title: In vivo effects of the IKr agonist NS3623 on cardiac electrophysiology of the guinea pig.

Journal: Journal of cardiovascular pharmacology 20080701

Title: Pharmacological separation of hEAG and hERG K+ channel function in the human mammary carcinoma cell line MCF-7.

Journal: Oncology reports 20080601

Title: Erg K+ channels modulate contractile activity in the bovine epididymal duct.

Journal: American journal of physiology. Regulatory, integrative and comparative physiology 20080301

Title: Characterization of the effects of ryanodine, TTX, E-4031 and 4-AP on the sinoatrial and atrioventricular nodes.

Journal: Progress in biophysics and molecular biology 20080101

Title: Aging-related changes of QT and RR intervals in conscious guinea pigs.

Journal: Journal of pharmacological and toxicological methods 20080101

Title: Fluorescently labeled analogues of dofetilide as high-affinity fluorescence polarization ligands for the human ether-a-go-go-related gene (hERG) channel.

Journal: Journal of medicinal chemistry 20070628

Title: Pharmacological activation of rapid delayed rectifier potassium current suppresses bradycardia-induced triggered activity in the isolated guinea pig heart.

Journal: The Journal of pharmacology and experimental therapeutics 20070601

Title: Identification of IKr and its trafficking disruption induced by probucol in cultured neonatal rat cardiomyocytes.

Journal: The Journal of pharmacology and experimental therapeutics 20070601

Title: Hydroxypropyl beta-cyclodextrins: a misleading vehicle for the in vitro hERG current assay.

Journal: Journal of cardiovascular pharmacology 20070501

Title: Role of reverse mode Na+/Ca2+ exchanger in the cardioprotection of metabolic inhibition preconditioning in rat ventricular myocytes.

Journal: European journal of pharmacology 20070430

Title: Functional effects of the late sodium current inhibition by AZD7009 and lidocaine in rabbit isolated atrial and ventricular tissue and Purkinje fibre.

Journal: European journal of pharmacology 20070308

Title: Temperature acclimation modifies sinoatrial pacemaker mechanism of the rainbow trout heart.

Journal: American journal of physiology. Regulatory, integrative and comparative physiology 20070201

Title: Evaluation of the guinea pig monophasic action potential (MAP) assay in predicting drug-induced delay of ventricular repolarisation using 12 clinically documented drugs.

Journal: Journal of pharmacological and toxicological methods 20070101

Title: Suitability of commonly used excipients for electrophysiological in-vitro safety pharmacology assessment of effects on hERG potassium current and on rabbit Purkinje fiber action potential.

Journal: Journal of pharmacological and toxicological methods 20070101

Title: Drug-induced long QT syndrome: hERG K+ channel block and disruption of protein trafficking by fluoxetine and norfluoxetine.

Journal: British journal of pharmacology 20061101

Title: Contribution of I Ks to ventricular repolarization in canine myocytes.

Journal: Pflugers Archiv : European journal of physiology 20060901

Title: Diabetes mellitus reduces the antiarrhythmic effect of ion channel blockers.

Journal: Anesthesia and analgesia 20060901

Title: Molecular determinants of HERG channel block.

Journal: Molecular pharmacology 20060501

Title: QT prolongation modifies dynamic restitution and hysteresis of the beat-to-beat QT-TQ interval relationship during normal sinus rhythm under varying states of repolarization.

Journal: The Journal of pharmacology and experimental therapeutics 20060201

Title: A novel predictive pharmacokinetic/pharmacodynamic model of repolarization prolongation derived from the effects of terfenadine, cisapride and E-4031 in the conscious chronic av node--ablated, His bundle-paced dog.

Journal: Journal of pharmacological and toxicological methods 20060101

Title: [Identification of E-4031-sensitive potassium current component in murine P19 embryonic carcinoma cell line differentiated in cardiomyocytes].

Journal: Fiziolohichnyi zhurnal (Kiev, Ukraine : 1994) 20060101

Title: Safety pharmacology assessment of drug-induced QT-prolongation in dogs with reduced repolarization reserve.

Journal: Journal of pharmacological and toxicological methods 20060101

Title: Dimethyl sulfoxide effects on hERG channels expressed in HEK293 cells.

Journal: Journal of pharmacological and toxicological methods 20060101

Title: Expression and functional phenotype of mouse ERG K+ channels in the inner ear: potential role in K+ regulation in the inner ear.

Journal: The Journal of neuroscience : the official journal of the Society for Neuroscience 20050921

Title: Practical application of guinea pig telemetry system for QT evaluation.

Journal: The Journal of toxicological sciences 20050801

Title: Novel mutation in the Per-Arnt-Sim domain of KCNH2 causes a malignant form of long-QT syndrome.

Journal: Circulation 20050301

Title: Cellular and ionic mechanism for drug-induced long QT syndrome and effectiveness of verapamil.

Journal: Journal of the American College of Cardiology 20050118

Title: Dynamic beat-to-beat modeling of the QT-RR interval relationship: analysis of QT prolongation during alterations of autonomic state versus human ether a-go-go-related gene inhibition.

Journal: The Journal of pharmacology and experimental therapeutics 20050101

Title: Expression of human ERG K+ channels in the mouse heart exerts anti-arrhythmic activity.

Journal: Cardiovascular research 20050101

Title: Estimation of potency of HERG channel blockers: impact of voltage protocol and temperature.

Journal: Journal of pharmacological and toxicological methods 20050101

Title: Electrophysiological effects of ranolazine, a novel antianginal agent with antiarrhythmic properties.

Journal: Circulation 20040824

Title: Antagonism by ranolazine of the pro-arrhythmic effects of increasing late INa in guinea pig ventricular myocytes.

Journal: Journal of cardiovascular pharmacology 20040801

Title: Structural determinants of HERG channel block by clofilium and ibutilide.

Journal: Molecular pharmacology 20040801

Title: Sevoflurane inhibition of the slowly activating delayed rectifier K+ current in guinea pig ventricular cells.

Journal: Journal of pharmacological sciences 20040701

Title: Epicardial activation of left ventricular wall prolongs QT interval and transmural dispersion of repolarization: implications for biventricular pacing.

Journal: Circulation 20040504

Title: A rapidly activating delayed rectifier K+ current regulates pacemaker activity in adult mouse sinoatrial node cells.

Journal: American journal of physiology. Heart and circulatory physiology 20040501

Title: Differential effect of HERG blocking agents on cardiac electrical alternans in the guinea pig.

Journal: European journal of pharmacology 20040220

Title: [High throughput screening method of potassium channel regulators].

Journal: Yao xue xue bao = Acta pharmaceutica Sinica 20040201

Title: HERG K channel conductance promotes H2O2-induced apoptosis in HEK293 cells: cellular mechanisms.

Journal: Cellular physiology and biochemistry : international journal of experimental cellular physiology, biochemistry, and pharmacology 20040101

Title: Effects of E4031 and quinidine on atrial and ventricular refractoriness in rabbits in vivo.

Journal: Proceedings of the Western Pharmacology Society 20040101

Title: ERG K+ currents regulate pacemaker activity in ICC.

Journal: American journal of physiology. Gastrointestinal and liver physiology 20031201

Title: Cardiovascular assessment of ER-118585, a selective phosphodiesterase 5 inhibitor.

Journal: Biological & pharmaceutical bulletin 20031201

Title: Role of K(+) channels in frequency regulation of spontaneous action potentials in rat pituitary GH(3) cells.

Journal: Neuroendocrinology 20031101

Title: Comparison of potassium currents in human decidua before and after the onset of labor.

Journal: Biology of reproduction 20030601

Title: Expression and function of KCNH2 (HERG) in the human jejunum.

Journal: American journal of physiology. Gastrointestinal and liver physiology 20030601

Title: Preserved effects of potassium channel blockers in the pacing-induced remodeled canine atrium: a comparison between E4031 and azimilide.

Journal: Journal of cardiovascular pharmacology 20030501

Title: Transmural heterogeneity of the action potential configuration in the feline left ventricle.

Journal: Circulation journal : official journal of the Japanese Circulation Society 20030501

Title: Dissociation of E-4031 from the HERG channel caused by mutations of an amino acid results in greater block at high stimulation frequency.

Journal: Cardiovascular research 20030301

Title: Cardiac electrophysiological modulation by NS-7, a novel neuroprotective drug, of guinea pig ventricular muscles.

Journal: Life sciences 20030117

Title: Block of erg current by linoleoylamide, a sleep-inducing agent, in pituitary GH3 cells.

Journal: European journal of pharmacology 20030101

Title: E-4031 enhanced Ca2+ transient and ventricular myocytes contraction via reverse mode Na+/Ca2+ exchange in normal and hypertrophic rats.

Journal: Acta pharmacologica Sinica 20020901

Title: The relationship of clinical QT prolongation to outcome in the conscious dog using a beat-to-beat QT-RR interval assessment.

Journal: The Journal of pharmacology and experimental therapeutics 20020801

Title: The binding site for channel blockers that rescue misprocessed human long QT syndrome type 2 ether-a-gogo-related gene (HERG) mutations.

Journal: The Journal of biological chemistry 20020215

Title: Molecular and functional characterization of ERG, KCNQ, and KCNE subtypes in rat stomach smooth muscle.

Journal: American journal of physiology. Gastrointestinal and liver physiology 20020201

Title: Prominent I(Ks) in epicardium and endocardium contributes to development of transmural dispersion of repolarization but protects against development of early afterdepolarizations.

Journal: Journal of cardiovascular electrophysiology 20020201

Title: Does lindane (gamma-hexachlorocyclohexane) increase the rapid delayed rectifier outward K+ current (IKr) in frog atrial myocytes?

Journal: BMC pharmacology 20020101

Title: Inhibitory effect of bepridil on hKv1.5 channel current: comparison with amiodarone and E-4031.

Journal: European journal of pharmacology 20011102

Title: Potassium channel blocker activates extracellular signal-regulated kinases through Pyk2 and epidermal growth factor receptor in rat cardiomyocytes.

Journal: Journal of the American College of Cardiology 20011101

Title: Effects of different types of K+ channel modulators on the spontaneous myogenic contraction of guinea-pig urinary bladder smooth muscle.

Journal: Acta physiologica Scandinavica 20011101

Title: Heterogeneous expression of the delayed-rectifier K+ currents i(K,r) and i(K,s) in rabbit sinoatrial node cells.

Journal: The Journal of physiology 20010915

Title: Density and kinetics of I(Kr) and I(Ks) in guinea pig and rabbit ventricular myocytes explain different efficacy of I(Ks) blockade at high heart rate in guinea pig and rabbit: implications for arrhythmogenesis in humans.

Journal: Circulation 20010821

Title: Rate dependency of delayed rectifier currents during the guinea-pig ventricular action potential.

Journal: The Journal of physiology 20010801

Title: Interactions between antiarrhythmic drugs and cardiac memory.

Journal: Cardiovascular research 20010501

Title: The slow component of the delayed rectifier potassium current in undiseased human ventricular myocytes.

Journal: Cardiovascular research 20010301

Title: Alosetron and the rapid component of delayed rectifying potassium current in cardiac cells.

Journal: Life sciences 20010223

Title: Differences in action potential and early afterdepolarization properties in LQT2 and LQT3 models of long QT syndrome.

Journal: British journal of pharmacology 20010101

Title: Pharmacological block of the slow component of the outward delayed rectifier current (I(Ks)) fails to lengthen rabbit ventricular muscle QT(c) and action potential duration.

Journal: British journal of pharmacology 20010101

Title: Pharmacokinetic/pharmacodynamic assessment of the effects of E4031, cisapride, terfenadine and terodiline on monophasic action potential duration in dog.

Journal: Xenobiotica; the fate of foreign compounds in biological systems 20010101

Title: Statistical analysis of QT interval as a function of changes in RR interval in the conscious dog.

Journal: Journal of pharmacological and toxicological methods 20010101

Title: Correction of defective protein trafficking of a mutant HERG potassium channel in human long QT syndrome. Pharmacological and temperature effects.

Journal: The Journal of biological chemistry 19991029

Title: Properties of HERG channels stably expressed in HEK 293 cells studied at physiological temperature.

Journal: Biophysical journal 19980101

Title: Daisuke Izumi, et al. Effects of bepridil versus E-4031 on transmural ventricular repolarization and inducibility of ventricular tachyarrhythmias in the dog. Pacing Clin Electrophysiol. 2010 Aug;33(8):950-9.

Title: E E Verheijck, et al. Effects of delayed rectifier current blockade by E-4031 on impulse generation in single sinoatrial nodal myocytes of the rabbit. Circ Res. 1995 Apr;76(4):607-15.

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