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ICA-27243

SKU: orb1219622

Description

ICA-27243 is less effective at activating KCNQ4 and KCNQ3/Q5. ICA-27243 is a potent and orally active KCNQ2/Q3 potassium channel opener (EC50: 0.38 μM). ICA-27243 also has antiepileptic and anticonvulsant effects. 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 .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).

Images & Validation

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ICA-27243

Key Properties

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CAS Number325457-89-4
MW268.65
Purity>98% (HPLC)
FormulaC12H7ClF2N2O
SMILESFc1ccc(cc1F)C(=O)Nc1ccc(Cl)nc1
TargetPotassium Channel
SolubilityDMSO:247 mg/mL (919.41mM; Need ultrasonic)

Bioactivity

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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. Animal model: Male CD-1 mice with electroshock assay. 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.
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).

Storage & Handling

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StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

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  • ICA-27243 [orb1308212]

    99.54% (May vary between batches)

    325457-89-4

    268.65

    C12H7ClF2N2O

    10 mg, 100 mg, 2 mg, 25 mg, 1 ml x 10 mM (in DMSO), 5 mg, 50 mg
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Gene Symbol
Potassium Channel

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