1. Membrane Transporter/Ion Channel
  2. Potassium Channel
  3. E-4031 free base

E-4031 free base is a selective hERG potassium channel blocker for use in class III anti-arrhythmic studies.

For research use only. We do not sell to patients.

CAS No. : 113558-89-7

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Top Publications Citing Use of Products

    E-4031 free base purchased from MedChemExpress. Usage Cited in: JCI Insight. 2025 Sep 30:e191697.  [Abstract]

    Western blot showing trafficked (fully glycosylated, ~155 kDa) and non-trafficked (core glycosylated, ~135 kDa) Kv11.1 protein. E4031 (10 μM; 24 h) increaseed trafficking in 2 variants.

    E-4031 free base purchased from MedChemExpress. Usage Cited in: J Mol Cell Biol. 2025 Jan 23:mjae051.  [Abstract]

    Representative whole-cell hERG currents in KCNH2-transfected HEK293T cells were recorded in the absence or presence of E-4031.

    E-4031 free base purchased from MedChemExpress. Usage Cited in: ACS Appl Mater Interfaces. 2023 Apr 12;15(14):17518-17531.  [Abstract]

    E-4031 (50-100 nM) obviously decreased beating frequency and velocity for hiPSC-CMs on glass, AN, and AN-MR substrates. The beating rate of hiPSC-CMs decreased by 32.33 and 45.55% on glass, 33.78 and 40.6% on AN group, and 33.29 and 35.59% on AN-MR group at 50 and 100 nM conditions, respectively.

    E-4031 free base purchased from MedChemExpress. Usage Cited in: Biofabrication. 2022 Oct 28;15(1).  [Abstract]

    E-4031 (50-100 nM) notably decreased the beating frequency when acting directly on the hiPSC-CMs layer (CM-static and CM-dynamic).

    E-4031 free base purchased from MedChemExpress. Usage Cited in: Toxicol Appl Pharmacol. 2021 Nov 15:431:115731.  [Abstract]

    For the field potential property of hiPSC-CMs cultured for 30 days, the onset of E-4031 (100 nM) was very quick, usually within 5 min. E-4031 significantly prolonged FPDc of hiPSC-CMs.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    E-4031 free base is a selective hERG potassium channel blocker for use in class III anti-arrhythmic studies[1].

    Cellular Effect
    Cell Line Type Value Description References
    CHO-K1 IC50
    0.024 μM
    Compound: E-4031
    Inhibition of human ERG expressed in CHOK1 cells assessed as inhibition of tail current after 5 mins by automated whole-cell patch clamp assay
    Inhibition of human ERG expressed in CHOK1 cells assessed as inhibition of tail current after 5 mins by automated whole-cell patch clamp assay
    [PMID: 27105029]
    COS-7 IC50
    10.2 nM
    Compound: E-4031
    Inhibition of hERG Voltage-gated potassium channel subunit Kv11.1 expressed in COS7 cells by electrophysiological whole cell assay
    Inhibition of hERG Voltage-gated potassium channel subunit Kv11.1 expressed in COS7 cells by electrophysiological whole cell assay
    [PMID: 15084130]
    HEK293 IC50
    0.027 μM
    Compound: E-4031
    Inhibition of human ERG expressed in HEK293 cells by patch clamp assay
    Inhibition of human ERG expressed in HEK293 cells by patch clamp assay
    [PMID: 32298114]
    Ventricular myocyte IC50
    441 μM
    Compound: E-4031
    Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
    Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
    [PMID: 22761000]
    Molecular Weight

    401.52

    Formula

    C21H27N3O3S

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CS(=O)(NC1=CC=C(C(C2CCN(CCC3=NC(C)=CC=C3)CC2)=O)C=C1)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (249.05 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.4905 mL 12.4527 mL 24.9054 mL
    5 mM 0.4981 mL 2.4905 mL 4.9811 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (6.23 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (6.23 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.4905 mL 12.4527 mL 24.9054 mL 62.2634 mL
    5 mM 0.4981 mL 2.4905 mL 4.9811 mL 12.4527 mL
    10 mM 0.2491 mL 1.2453 mL 2.4905 mL 6.2263 mL
    15 mM 0.1660 mL 0.8302 mL 1.6604 mL 4.1509 mL
    20 mM 0.1245 mL 0.6226 mL 1.2453 mL 3.1132 mL
    25 mM 0.0996 mL 0.4981 mL 0.9962 mL 2.4905 mL
    30 mM 0.0830 mL 0.4151 mL 0.8302 mL 2.0754 mL
    40 mM 0.0623 mL 0.3113 mL 0.6226 mL 1.5566 mL
    50 mM 0.0498 mL 0.2491 mL 0.4981 mL 1.2453 mL
    60 mM 0.0415 mL 0.2075 mL 0.4151 mL 1.0377 mL
    80 mM 0.0311 mL 0.1557 mL 0.3113 mL 0.7783 mL
    100 mM 0.0249 mL 0.1245 mL 0.2491 mL 0.6226 mL
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
    E-4031 free base
    Cat. No.:
    HY-15551A
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