ICA-27243

Product details

• Chemical name: N-(6-Chloro-pyridin-3-yl)-3,4-difluoro-benzamide.
• CAS number: 325457-89-4
• Molecular formula: C12H7ClF2N2O.
• Purity: >99%
• Concentration: 0.5-50 µM.
• Form: Lyophilized powder.
• Solubility: 100 mM DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
• Reconstitution: Centrifuge the vial before adding solvent (10,000 x g for 5 minutes) to spin down all the powder to the bottom of the vial. The lyophilized product may be difficult to visualize. Add solvent directly to the centrifuged vial. Tap the vial to aid in dissolving the lyophilized product. Tilt and gently roll the liquid over the walls of the vial. Avoid vigorous vortexing. Light vortexing for up to 3 seconds is acceptable if needed. Soluble in water. Once dissolved in water, add an equal volume of glycerol. Do not shake or vortex. Avoid multiple freeze-thawing cycles
• Shipping: 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.
• Target: KCNQ2, KCNQ3 K+ channels
• Source: Synthetic
• Activity: ICA-27243 is a potent and selective KCNQ channel modulator (enhancer)1 with EC50 ~ 1 µM.

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.

Lead time: 1-2 Business Days

Country of origin: Israel/IL

Applications key

Application key: FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay.

Bioassay tested: Yes

• SDS (PDF)

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