Art. -Nr.: HY-15551A

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E-4031 free base

8 Cited Publications

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

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Reinheit: 98.92%
CAS. Nr.: 113558-89-7
Formel: C₂₁H₂₇N₃O₃S
Molecular Weight:401.52

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

E-4031 free base Chemical Structure

CAS. Nr.: 113558-89-7

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Biologische Aktivität
- Beschreibung
- Cellular Effect
Chemical Information
Publications (8)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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]
Vero C1008	IC₅₀	>2.0 × 10⁵M Compound: COVC-3899201806	Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging	10.6019/CHEMBL4651402

Chemical Information

CAS. Nr. 113558-89-7
Appearance Solid
Molecular Weight 401.52
Formel C₂₁H₂₇N₃O₃S
Color White to off-white
SMILES

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

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (8)

All Bio/Physico-chemical AssayWB

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Journal Impact Factor

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 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).
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 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.
JCI Insight

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

2025 Sep 30:e191697. PMID: 41026531

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.
J Mol Cell Biol

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

2025 May 22;16(11):mjae051. PMID: 39848918

E-4031 free base purchased from MedChemExpress. Usage Cited in: J Mol Cell Biol. 2025 May 22;16(11):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 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.
bioRxiv

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

2026 Feb 13:2026.02.11.705466. PMID: 41727060

Lösungsmittel & Löslichkeit

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)

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

2.4905 mL

12.4527 mL

24.9054 mL

5 mM

0.4981 mL

2.4905 mL

4.9811 mL

10 mM

0.2491 mL

1.2453 mL

2.4905 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, 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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)
Handling Instructions (2659 KB)

Verweise

[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

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

Keywords

E-4031 free base

8 Cited Publications

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E-4031 free base

Anti-Cardiovascular Disease Compound Library

Anti-Alzheimer's Disease Compound Library

Neurodegenerative Disease-related Compound Library

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Human Metabolite 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

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Membrane Transporter/Ion Channel Compound Library

Publications Citing Use of MedChemExpress (MCE) E-4031 free base

Biologische Aktivität

Chemical Information

Publications (8)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

E-4031 free base

Anti-Cardiovascular Disease Compound Library

Anti-Alzheimer's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Potassium Channel Compound Library

Human Metabolite 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

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Membrane Transporter/Ion Channel Compound Library

Publications Citing Use of MedChemExpress (MCE) E-4031 free base

Biologische Aktivität

Chemical Information

Publications (8)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

E-4031 free base Related Classifications

HY-15551A Related Classifications