Gavestinel (sodium salt)

Gavestinel is an NMDA receptor antagonist. It selectively binds to the glycine site of the NMDA receptor over the glutamate binding site of NMDA, AMPA, or ionotropic kainate (GluK) receptors (Kis = 0.003, 10, 7.94, and 3.98 µM, respectively) and is selective for the NMDA receptor over a panel of 70 receptors (IC50s = >10 µM for all). Gavestinel (0.03-0.35 µM) inhibits glutamate-induced increases in intracellular calcium levels in primary rat neonatal cerebral cortical neurons. It reduces infarct volume in a rat model of focal ischemia induced by middle cerebral artery occlusion (MCAO) when administered intravenously at a dose of 3 mg/kg.Formal Name: 4,6-dichloro-3-[(1E)-3-oxo-3-(phenylamino)-1-propen-1-yl]-1H-indole-2-carboxylic acid, monosodium salt. CAS Number: 153436-38-5. Synonyms: GV150526A. Molecular Formula: C18H11Cl2N2O3 . Na. Formula Weight: 397.2. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble. SMILES: O=C(NC1=CC=CC=C1)/C=C/C2=C(C([O-])=O)NC3=CC(Cl)=CC(Cl)=C23.[Na+]. InChi Code: InChI=1S/C18H12Cl2N2O3.Na/c19-10-8-13(20)16-12(17(18(24)25)22-14(16)9-10)6-7-15(23)21-11-4-2-1-3-5-11,/h1-9,22H,(H,21,23)(H,24,25),/q,+1/p-1/b7-6+,. InChi Key: GRSDSTMFQHAESM-UHDJGPCESA-M.