Cat. No.: HY-15551

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E-4031

8 Cited Publications

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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.

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Pureté: 99.40%
CAS No.: 113559-13-0
Formule: C₂₁H₂₉Cl₂N₃O₃S
Masse moléculaire:474.44

Stockage:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

E-4031 Chemical Structure

CAS No.: 113559-13-0

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Activité biologique
- Description
- Cellular Effect
- In Vitro
Chemical Information
Publications (8)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

E-4031 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	IC₅₀	89 nM Compound: E-4031	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	[PMID: 24805037]
CHO	IC₅₀	89 nM Compound: E-4031	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	[PMID: 25557493]
HEK293	IC₅₀	0.02 μM Compound: 1, E-4031	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	[PMID: 19260734]
HEK293	IC₅₀	0.02 μM Compound: 1, E-4031	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	[PMID: 19260734]
HEK293	IC₅₀	0.25 μM Compound: 1, E-4031	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	[PMID: 19260734]
HEK293	IC₅₀	0.69 μM Compound: 1, E-4031	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	[PMID: 19260734]
HEK293	IC₅₀	2.95 μM Compound: 1, E-4031	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	[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	[PMID: 19260734]

In Vitro

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 (I_TD) during subsequent repolarization in a dose-dependent manner, and depresses I_TD 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.

Chemical Information

CAS No. 113559-13-0
Appearance Solid
Masse moléculaire 474.44
Formule C₂₁H₂₉Cl₂N₃O₃S
Color White to off-white
SMILES

CS(=O)(NC1=CC=C(C(C2CCN(CCC3=NC(C)=CC=C3)CC2)=O)C=C1)=O.[H]Cl.[H]Cl
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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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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).
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.
JCI Insight

High throughput screens identify genotype-specific therapeutics for channelopathies. [Abstract]

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.
J Mol Cell Biol

Low-dose quinine targets KCNH6 to potentiate glucose-induced insulin secretion. [Abstract]

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.
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.
bioRxiv

Human-engineered heart tissues recapitulate tissue-scale mechanisms underlying ventricular tachycardia. [Abstract]

2026 Feb 13:2026.02.11.705466. PMID: 41727060

Solvant et solubilité

In Vitro:

H₂O : ≥ 50 mg/mL (105.39 mM)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1077 mL

10.5387 mL

21.0775 mL

5 mM

0.4215 mL

2.1077 mL

4.2155 mL

10 mM

0.2108 mL

1.0539 mL

2.1077 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Working Solution

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.

Protocol 1

Add each solvent one by one: PBS

Solubility: 100 mg/mL (210.77 mM); Clear solution; Need ultrasonic

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (272 KB)
SDS (392 KB)
- English - EN (392 KB)
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- 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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

Keywords

E-4031

8 Cited Publications

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E-4031

Membrane Transporter/Ion Channel Compound Library

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Anti-Cardiovascular Disease Compound Library

Anti-Alzheimer's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Potassium Channel Compound Library

Human Metabolite Library

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Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

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High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Cardiotoxic Compound Library

RNA Binding Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) E-4031

Activité biologique

Chemical Information

Publications (8)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

E-4031

Membrane Transporter/Ion Channel Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Anti-Cardiovascular Disease Compound Library

Anti-Alzheimer's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Potassium Channel Compound Library

Human Metabolite Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Cardiotoxic Compound Library

RNA Binding Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) E-4031

Activité biologique

Chemical Information

Publications (8)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

E-4031 Related Classifications

HY-15551 Related Classifications