For research use only. Not for therapeutic Use.
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].
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].
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].
| Catalog Number | I007250 |
| CAS Number | 325457-89-4 |
| Synonyms | N-(6-chloropyridin-3-yl)-3,4-difluorobenzamide |
| Molecular Formula | C12H7ClF2N2O |
| Purity | ≥95% |
| InChI | InChI=1S/C12H7ClF2N2O/c13-11-4-2-8(6-16-11)17-12(18)7-1-3-9(14)10(15)5-7/h1-6H,(H,17,18) |
| InChIKey | GDGUOCFTHNGPBK-UHFFFAOYSA-N |
| SMILES | C1=CC(=C(C=C1C(=O)NC2=CN=C(C=C2)Cl)F)F |
| Reference | [1]. Wickenden AD, et al. N-(6-chloro-pyridin-3-yl)-3,4-difluoro-benzamide (ICA-27243): a novel, selective KCNQ2/Q3 potassium channel activator. Mol Pharmacol. 2008 Mar;73(3):977-86. [2]. Amato G, et al. N-Pyridyl and Pyrimidine Benzamides as KCNQ2/Q3 Potassium Channel Openers for the Treatment of Epilepsy. ACS Med Chem Lett. 2011 Mar 31;2(6):481-4. |
