ICA-27243 是选择性的，口服有效的KCNQ2/Q3钾通道开放剂，EC50为 0.38 μM。对 KCNQ4 和 KCNQ3/Q5 的激活效果较差。它具有抗惊厥和抗癫痫作用。

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 [1].

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)[1].

325457-89-4

C12H7ClF2N2O

268.65

DMSO:247 mg/mL (919.41mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years