E-4031 dihydrochloride

SKU: orb1299987

Description

E-4031

Research Area

Cardiovascular Research, Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 113559-13-0
• MW: 474.44
• Purity: 99.31%
• 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