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E-4031

Catalog No. T7198   CAS 113559-13-0

E-4031 is a methanesulfonanilide class III antiarrhythmic agent that prolongs cardiac action potential duration by blocking ERG K+ channels (IC50 = 29 nM)

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E-4031 Chemical Structure
E-4031, CAS 113559-13-0
Pack Size Availability Price/USD Quantity
2 mg In stock $ 38.00
5 mg In stock $ 61.00
10 mg In stock $ 97.00
25 mg In stock $ 229.00
50 mg In stock $ 412.00
100 mg In stock $ 613.00
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Purity: 97.71%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description E-4031 is a methanesulfonanilide class III antiarrhythmic agent that prolongs cardiac action potential duration by blocking ERG K+ channels (IC50 = 29 nM)
Targets&IC50 ERG K+ channel (human):29 nM
In vivo At baseline, APD was longer in LQT1 than in LMC rabbits in LV apex and RV mid. Erythromycin and E-4031prolonged APD in LQT1 and LMC rabbits in all positions. However, erythromycin-induced percentaged APD prolongation related to baseline (%APD) was more pronounced in LQT1 at LV base-lateral and RV mid positions (100 μM, LQT1, +40.6 ± 9.7% vs. LMC, +24.1 ± 10.0%, p<0.05) and E-4031-induced %APD prolongation was more pronounced in LQT1 at LV base-lateral (0.01 μM, LQT1, +29.6 ± 10.6% vs. LMC, +19.1 ± 3.8%, p<0.05) and LV base-septal positions. Moreover, erythromycin significantly increased spatial APD dispersion only in LQT1 and increased triangulation only in LQT1 in LV base-septal and RV mid positions. Similarly, E-4031 increased triangulation only in LQT1 in LV apex and base-septal positions[1]
Animal Research Hearts of adult female transgenic LQT1 and wild type littermate control (LMC) rabbits were Langendorff-perfused with increasing concentrations of HERG/IKr-blockers E-4031 (0.001-0.1 μM, n=9/7) and APD, APD dispersion, and triangulation were analyzed[1].
Molecular Weight 474.44
Formula C21H29Cl2N3O3S
CAS No. 113559-13-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 50 mg/mL (105.39 mM)

TargetMolReferences and Literature

1. David Z , Julia B , Gerlind F , et al. Pronounced Effects of HERG-Blockers E-4031 and Erythromycin on APD, Spatial APD Dispersion and Triangulation in Transgenic Long-QT Type 1 Rabbits[J]. PLoS ONE, 2014, 9(9):e107210-. 2. Nalos L , Varkevisser R , Jonsson M K B , et al. Comparison of the IKr blockers moxifloxacin, dofetilide and E-4031 in five screening models of pro-arrhythmia reveals lack of specificity of isolated cardiomyocytes[J]. British Journal of Pharmacology, 2011, 165(2):467-478.

Related compound libraries

This product is contained In the following compound libraries:
Tyrosine Kinase Inhibitor Library Kinase Inhibitor Library Membrane Protein-targeted Compound Library JAK-STAT Compound Library Anti-Liver Cancer Compound Library Anti-Cancer Compound Library Angiogenesis related Compound Library Reprogramming Compound Library Ion Channel Inhibitor Library Anti-COVID-19 Compound Library

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Keywords

E-4031 113559-13-0 Angiogenesis JAK/STAT signaling Membrane transporter/Ion channel Tyrosine Kinase/Adaptors EGFR Potassium Channel Inhibitor anti-arrhythmic E4031 KcsA inhibit hERG E 4031 inhibitor

 

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