E-4031
Based on 8 publication(s) in Google Scholar
E-4031 is a selective hERG potassium channel blocker for use in class III anti-arrhythmic studies.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.40%
- CAS 番号: 113559-13-0
- 分子式: C21H29Cl2N3O3S
- 分子量:474.44
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
MedChemExpress(MCE)の使用を引用している文献 E-4031
More- Biofabrication. 2022 Oct 28;15(1). [Abstract]
- Free Radic Biol Med. 2026 Jun:249:14-26. [Abstract]
- ACS Appl Mater Interfaces. 2023 Apr 12;15(14):17518-17531. [Abstract]
- JCI Insight. 2025 Sep 30:e191697. [Abstract]
- J Mol Cell Biol. 2025 Jan 23:mjae051. [Abstract]
- Int J Mol Sci. 2026 Apr 21;27(8):3701. [Abstract]
- Toxicol Appl Pharmacol. 2021 Nov 15:431:115731. [Abstract]
- bioRxiv. 2026 Feb 13:2026.02.11.705466. [Abstract]
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WB
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
89 nM
Compound: E-4031
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Inhibition of human cloned ERG expressed in CHO cells assessed as inhibition of potassium channel current by automated patch clamp assay
Inhibition of human cloned ERG expressed in CHO cells assessed as inhibition of potassium channel current by automated patch clamp assay
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[PMID: 24805037] |
| CHO | IC50 |
89 nM
Compound: E-4031
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Inhibition of human ERG expressed in CHO cells assessed as reduction in channel current at holding potential of 0 mV by electrophysiological method
Inhibition of human ERG expressed in CHO cells assessed as reduction in channel current at holding potential of 0 mV by electrophysiological method
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[PMID: 25557493] |
| HEK293 | IC50 |
0.02 μM
Compound: 1, E-4031
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Inhibition of human ERG td[wt:F656A] mutant expressed in HEK293 cells by whole cell patch clamp method
Inhibition of human ERG td[wt:F656A] mutant expressed in HEK293 cells by whole cell patch clamp method
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[PMID: 19260734] |
| HEK293 | IC50 |
0.02 μM
Compound: 1, E-4031
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Inhibition of wild-type human ERG expressed in HEK293 cells by whole cell patch clamp method
Inhibition of wild-type human ERG expressed in HEK293 cells by whole cell patch clamp method
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[PMID: 19260734] |
| HEK293 | IC50 |
0.25 μM
Compound: 1, E-4031
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Inhibition of human ERG td[wt:Y652A] mutant expressed in HEK293 cells by whole cell patch clamp method
Inhibition of human ERG td[wt:Y652A] mutant expressed in HEK293 cells by whole cell patch clamp method
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[PMID: 19260734] |
| HEK293 | IC50 |
0.69 μM
Compound: 1, E-4031
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Inhibition of human ERG S624A mutant expressed in HEK293 cells by whole cell patch clamp method
Inhibition of human ERG S624A mutant expressed in HEK293 cells by whole cell patch clamp method
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[PMID: 19260734] |
| HEK293 | IC50 |
2.95 μM
Compound: 1, E-4031
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Inhibition of human ERG F656A mutant expressed in HEK293 cells by whole cell patch clamp method
Inhibition of human ERG F656A mutant expressed in HEK293 cells by whole cell patch clamp method
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[PMID: 19260734] |
| HEK293 | IC50 |
6.78 μM
Compound: 1, E-4031
|
Inhibition of human ERG Y652A mutant expressed in HEK293 cells by whole cell patch clamp method
Inhibition of human ERG Y652A mutant expressed in HEK293 cells by whole cell patch clamp method
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[PMID: 19260734] |
E-4031 (0.1-10 μM) significantly depolarises the maximum diastolic potential (MDP) and prolongs the action charge that depolarises MDP from -58.8+0.9 to -24.5±1.8 mV at 1 μM and from -58.2±2.1 to -19.6±1.8 mV at 10 μM in single SAN cells of New Zealand albinc rabbits[2].
E-4031 (0.1-10 μM) can block part of the outward current during the depolarisation step as well as the tail current (ITD) during subsequent repolarization in a dose-dependent manner, and depresses ITD by 88 % at 10 μM in single SAN cells of New Zealand albinc rabbits[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 113559-13-0
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性状 Solid
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分子量 474.44
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分子式 C21H29Cl2N3O3S
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Color White to off-white
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SMILES
CS(=O)(NC1=CC=C(C(C2CCN(CCC3=NC(C)=CC=C3)CC2)=O)C=C1)=O.[H]Cl.[H]Cl
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
Publications (8)
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Journal Impact Factor
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Most Recent
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Biofabrication
Heart-on-a-chip using human iPSC-derived cardiomyocytes with integrated vascular endothelial layer based on culture patch as a potential platform for drug evaluation. [Abstract]2022 Oct 28;15(1). PMID: 36195063
E-4031 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).
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Free Radic Biol Med
Repurposing the hERG activator NS-1643 as a ferroptosis-targeting therapeutic against doxorubicin cardiotoxicity. [Abstract]2026 Jun:249:14-26. PMID: 41794151 -
ACS Appl Mater Interfaces
Aligned Nanofibrous Net Deposited Perpendicularly on Microridges Supports Endothelium Formation and Promotes the Structural Maturation of hiPSC-Derived Cardiomyocytes. [Abstract]2023 Apr 12;15(14):17518-17531. PMID: 36992621
E-4031 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.
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JCI Insight
2025 Sep 30:e191697. PMID: 41026531
E-4031 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.
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J Mol Cell Biol
2025 Jan 23:mjae051. PMID: 39848918
E-4031 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.
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Int J Mol Sci
Establishment and Characterization of a Stable hERG Cell Line for High-Throughput Drug Cardiac Safety Screening. [Abstract]2026 Apr 21;27(8):3701. PMID: 42074339 -
Toxicol Appl Pharmacol
Proarrhythmic effects induced by benzethonium chloride and domiphen bromide in vitro and in vivo. [Abstract]2021 Nov 15:431:115731. PMID: 34592322
E-4031 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.
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bioRxiv
Human-engineered heart tissues recapitulate tissue-scale mechanisms underlying ventricular tachycardia. [Abstract]2026 Feb 13:2026.02.11.705466. PMID: 41727060
溶剤 & 溶解度
H2O : ≥ 50 mg/mL (105.39 mM)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (210.77 mM); Clear solution; Need ultrasonic
純度とドキュメンテーション
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データシート (272 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. 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. [Content Brief]
[2]. 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. [Content Brief]
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, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 2.1077 mL | 10.5387 mL | 21.0775 mL | 52.6937 mL |
| 5 mM | 0.4215 mL | 2.1077 mL | 4.2155 mL | 10.5387 mL | |
| 10 mM | 0.2108 mL | 1.0539 mL | 2.1077 mL | 5.2694 mL | |
| 15 mM | 0.1405 mL | 0.7026 mL | 1.4052 mL | 3.5129 mL | |
| 20 mM | 0.1054 mL | 0.5269 mL | 1.0539 mL | 2.6347 mL | |
| 25 mM | 0.0843 mL | 0.4215 mL | 0.8431 mL | 2.1077 mL | |
| 30 mM | 0.0703 mL | 0.3513 mL | 0.7026 mL | 1.7565 mL | |
| 40 mM | 0.0527 mL | 0.2635 mL | 0.5269 mL | 1.3173 mL | |
| 50 mM | 0.0422 mL | 0.2108 mL | 0.4215 mL | 1.0539 mL | |
| 60 mM | 0.0351 mL | 0.1756 mL | 0.3513 mL | 0.8782 mL | |
| 80 mM | 0.0263 mL | 0.1317 mL | 0.2635 mL | 0.6587 mL | |
| 100 mM | 0.0211 mL | 0.1054 mL | 0.2108 mL | 0.5269 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.