E-4031 dihydrochloride

SKU: orb1299987

Description

E-4031 dihydrochloride is a potent and selective class III antiarrhythmic agent that blocks the ERG potassium channel (IC50 = 29 nM), thereby prolonging the cardiac action potential. It is widely used in cardiovascular research to study long QT syndrome and arrhythmia mechanisms in both cellular electrophysiology and isolated tissue experiments.

Research Area

Cardiovascular Research, Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 113559-13-0
• MW: 474.44
• Purity: 99.87% (May vary between batches)
• Formula: C₂₁H₂₉Cl₂N₃O₃S
• SMILES: Cl.Cl.Cc1cccc(CCN2CCC(CC2)C(=O)c2ccc(NS(C)(=O)=O)cc2)n1
• Target: EGFR,Potassium Channel
• Solubility: H2O:135 mg/mL (284.55 mM)

Bioactivity

• Target 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
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Potassium Channel, PotassiumChannel, hERG, hERG Potassium Channel, KcsA, inhibit, Inhibitor, E 4031, E4031, E-4031, anti-arrhythmic

Compound Identifiers

PubChem CID

3087190