ICA 27243

ICA 27243 is an activator of heteromeric voltage-gated potassium channels containing Kv7.2 and Kv7.3 subunits (Kv7.2/Kv7.3). It enhances rubidium efflux in an agonist-induced rubidium efflux assay using CHO cells expressing Kv7.2/Kv7.3 channels (EC50 = 0.38 µM). ICA 27243 is selective for heteromeric Kv7.2/Kv7.3 channels over homomeric Kv7.4 channels (EC50 = 7.1 µM) and is 100-300-fold selective for Kv7.2/Kv7.3 over Kv7.3/Kv7.5 channels. It is also selective for Kv7.2/Kv7.3 channels over a panel of neurotransmitter receptors and voltage-gated sodium channel Nav1.2 at 10 µM, as well as GABAA receptors and high voltage-activated calcium channels at 30 µM. ICA 27243 protects against maximal electroshock-induced seizures in a rat model of epilepsy (ED50 = 1.5 mg/kg). It also prevents hyperactivity induced by amphetamine and chlordiazepoxide, but not by amphetamine alone, without affecting basal locomotor activity in a mouse model of manic-like hyperactivity when administered at a dose of 10 mg/kg.Formal Name: N-(6-chloro-3-pyridinyl)-3,4-difluoro-benzamide. CAS Number: 325457-89-4. Synonyms: ICA 027243. Molecular Formula: C12H7ClF2N2O. Formula Weight: 268.7. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble: >10 mg/ml, Ethanol: Sparingly Soluble: 1-10 mg/ml. SMILES: O=C(C1=CC=C(C(F)=C1)F)NC2=CN=C(C=C2)Cl. InChi Code: 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). InChi Key: GDGUOCFTHNGPBK-UHFFFAOYSA-N.