1. Membrane Transporter/Ion Channel
  2. Potassium Channel
  3. ICA-27243

ICA-27243 

Cat. No.: HY-122114
Handling Instructions

ICA-27243 is a selective, potent and orally active KCNQ2/Q3 potassium channel opener with an EC50 of 0.38 μM. ICA-27243 is less effective at activating KCNQ4 and KCNQ3/Q5. ICA-27243 has antiepileptic and anticonvulsant effects.

For research use only. We do not sell to patients.

ICA-27243 Chemical Structure

ICA-27243 Chemical Structure

CAS No. : 325457-89-4

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Description

ICA-27243 is a selective, potent and orally active KCNQ2/Q3 potassium channel opener with an EC50 of 0.38 μM. ICA-27243 is less effective at activating KCNQ4 and KCNQ3/Q5. ICA-27243 has antiepileptic and anticonvulsant effects[1][2].

IC50 & Target

EC50: 0.38 μM (KCNQ2/Q3 potassium channel)[2]

In Vitro

In SH-SY5Y human neuroblastoma cells, ICA-27243 produces membrane potential hyperpolarization that could be prevented by coadministration with the M-current inhibitors XE-991 and Linopirdine. ICA-27243 enhances 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). Activation of KCNQ2/Q3 channels is associated with a hyperpolarizing shift of the voltage dependence of channel activation (V1/2 shift of -19 mV at 10 μM)[1].

In Vivo

ICA-27243 (1-100 mg/kg; oral administration; male CD-1 mice) has anticonvulsant activity (ED50 of 8.4 mg/kg) in the mouse maximal electroshock epilepsy model[1].

Animal Model: Male CD-1 mice with electroshock assay[1]
Dosage: 1-100 mg/kg
Administration: Oral administration
Result: Produced a dose-dependent increase in the latency to hind limb extension, exhibiting an ED50 value of 8.4 mg/kg.
Molecular Weight

268.65

Formula

C₁₂H₇ClF₂N₂O

CAS No.

325457-89-4

SMILES

O=C(C1=CC=C(C(F)=C1)F)NC2=CC=C(N=C2)Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

ICA-27243ICA27243ICA 27243Potassium ChannelKcsAKCNQ2KCNQ3openerantiepilepticanticonvulsanthyperpolarizationInhibitorinhibitorinhibit

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ICA-27243
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