ICA-27243

SKU: orb1308212

Description

ICA-27243 is a potent, orally bioavailable opener of KCNQ2/Q3 potassium channels (EC50: 0.38 µM) with demonstrated antiepileptic activity in animal models. It shows reduced efficacy on KCNQ4 and KCNQ3/Q5 channels, making it a selective tool for researching neuronal excitability and neuropathic pain in vitro and in vivo.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 325457-89-4
• MW: 268.65
• Purity: 99.79%
• Formula: C₁₂H₇ClF₂N₂O
• SMILES: Fc1ccc(cc1F)C(=O)Nc1ccc(Cl)nc1
• Target: Potassium Channel
• Solubility: DMSO:247 mg/mL (919.41 mM);10% DMSO+90% Corn Oil:3.3 mg/mL (12.28 mM)

Bioactivity

• Target IC50:
  KCNQ2/Q3 K+ channel:0.38 μM (EC50)
• In Vivo:
  In the mouse maximal electroshock epilepsy model, ICA-27243 (1-100 mg/kg; oral administration; male CD-1 mice) has anticonvulsant activity (ED50: 8.4 mg/kg).
• In Vitro:
  ICA-27243 increases both 86Rb+ efflux (EC50 = 0.2 μM) and whole-cell currents in Chinese hamster ovary cells stably expressing heteromultimeric KCNQ2/Q3 channels (EC50 = 0.4 μM). ICA-27243 produces membrane potential hyperpolarization that could be prevented by coadministration with the M-current inhibitors XE-991 and Linopirdine, in SH-SY5Y human neuroblastoma cells .

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, KCNQ3, KCNQ2/Q3 potassium channel, KCNQ2, inhibit, Inhibitor, KcsA, opener, hyperpolarization, ICA-27243, ICA27243, ICA 27243, antiepileptic, anticonvulsant

Compound Identifiers

PubChem CID

9903497