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

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 2 mg | $38 | In Stock | In Stock | |
| 5 mg | $61 | In Stock | In Stock | |
| 10 mg | $97 | In Stock | In Stock | |
| 25 mg | $229 | In Stock | In Stock | |
| 50 mg | $412 | In Stock | In Stock | |
| 100 mg | $613 | In Stock | In Stock |
| 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) |
| 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 |
| Smiles | Cl.Cl.Cc1cccc(CCN2CCC(CC2)C(=O)c2ccc(NS(C)(=O)=O)cc2)n1 |
| Relative Density. | no data available |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | H2O: 135 mg/mL (284.55 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
H2O
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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