Overview
ICA-27243 (#I-130) is a highly pure, synthetic, and biologically active compound.
Structure
For research purposes only, not for human use
Applications
Citations (2)
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Properties
Technical Specifications
MW 268.64
Purity >99%
Molecular formula C12H7ClF2N2O.
CAS No. 325457-89-4
Source Synthetic
PubChem CID 9903497
Chemical name N-(6-Chloro-pyridin-3-yl)-3,4-difluoro-benzamide.
Biological Activity
Target KCNQ2, KCNQ3 K+ channels
Effective concentration 0.5-50 µM.
Activity ICA-27243 is a potent and selective KCNQ channel modulator (enhancer)1 with EC50 ~ 1 µM.
References
- Padilla, K. et al. (2009) Neurosci. Lett. 465, 138.
Solubility and Storage
Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Solubility 100 mM DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
Storage of solutions Up to four weeks at 4°C or three months at -20°C.
Scientific Background
References
Scientific background KCNQ2 (KV7.2) and KCNQ3 (KV7.3) are voltage-gated K+ channel subunits that underlie the neuronal M current. ICA-27243 is a novel, potent and selective activator of M-current and KCNQ2/Q3 channels. ICA-27243 is structurally distinct from other known KCNQ/M-current activators. It enhances KCNQ channel activation by shifting channel opening to more hyperpolarized potentials. ICA-27243 activates KCNQ currents in Chinese hamster ovary cells expressing recombinant KCNQ2/Q3 heteromultimeric channels with an EC50 of 0.4 μM. ICA-27243 exhibits selectivity for KCNQ2/Q3 over KCNQ4 (20-fold) and KCNQ3/Q5 (>100-fold) and has no effect on GABA-activated chloride channels, neuronal Na+ channels, or voltage-gated Ca2+ channels. In addition, it produces minimal displacement of radioligand binding to a range of central nervous system receptors and transporters. ICA-27243 also suppresses seizure-like activity in an ex vivo hippocampal slice model, and protects against maximal electroshock-induced seizures in mice1.
References
- Wickenden, A.D. et al. (2008) Mol. Pharmacol. 73, 977.
Last Update: 08/01/2025
