ICA-27243 (ICA-207243) is a potent, selective KCNQ2/Q3 (Kv7.2/Kv7.3) potassium channel opener/activator with EC50 of 0.38 uM.
ICA-27243 enhances both (86)Rb(+) efflux (EC50= 0.2 microM) and whole-cell currents in CHO cells stably expressing heteromultimeric KCNQ2/Q3 channels (EC50= 0.4 microM).
ICA-27243 is less effective at activating KCNQ4 and KCNQ3/Q5 and is selective over a wide range of neurotransmitter receptors and ion channels such as voltage-dependent sodium channels and GABA-gated chloride channels.
ICA-27243 (1-10 microM) reversibly suppresses seizure-like activity in an ex vivo hippocampal slice model of epilepsy and demonstrates in vivo anticonvulsant activity (ED(50) = 8.4 mg/kg) in the mouse maximal electroshock epilepsy model.
Physicochemical Properties
M.Wt
268.648
Formula
C12H7ClF2N2O
Appearance
Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility
10 mM in DMSO
Chemical Name/SMILES
N-(6-chloro-pyridin-3-yl)-3,4-difluoro-benzamide
References
1. Amato G, et al. ACS Med Chem Lett. 2011 Mar 31;2(6):481-4.
