| Name | E-4031 dihydrochloride |
| Description | E-4031 dihydrochloride is a methanesulfonanilide class III antiarrhythmic agent that prolongs cardiac action potential duration by blocking ERG K+ channels (IC50 = 29 nM) |
| 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]. |
| 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] |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | H2O : 135 mg/mL (284.55 mM), Sonication is recommended.
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| Keywords | PotassiumChannel | Potassium Channel | KcsA | Inhibitor | inhibit | hERG Potassium Channel | hERG | E-4031 | E4031 | E 4031 | anti-arrhythmic |
| Inhibitors Related | Minoxidil sulfate | Tannic acid | Hydrochlorothiazide | 1,8-Cineole | Tetraethylammonium bromide | Ursodeoxycholic acid | Erlotinib | Chenodeoxycholic acid | Gefitinib | Chlorzoxazone | 2,2,2-Trichloroethanol | Indapamide |
| Related Compound Libraries | Pain-Related Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Angiogenesis related Compound Library | Stem Cell Differentiation Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Potassium Channel Targeted Library | Ion Channel Targeted Library | Anti-Cancer Compound Library |
United States
