ICA-27243

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

ICA-27243 激活 KCNQ4 和 KCNQ3/Q5 的效果较差。 ICA-27243 是一种有效的口服活性 KCNQ2/Q3 钾通道开放剂 (EC50: 0.38 μM)。

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).

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).

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.

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Cell Cycle/DNA Damage

Potassium Channel

KCNQ2/Q3 potassium channel

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325457-89-4

268.65

C12H7ClF2N2O

>98% (HPLC)

DMSO:247 mg/mL (919.41mM; Need ultrasonic)

Fc1ccc(cc1F)C(=O)Nc1ccc(Cl)nc1

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(-20℃)

With Ice Pack

≥ 2 years