CGP 3466 (maleate)

CGP 3466 is a GAPDH ligand. Immobilized CGP 3466 binds to GAPDH from rat hippocampus extracts and to purified recombinant rabbit muscle GAPDH using affinity purification. CGP 3466 reduces PAJU cell apoptosis induced by rotenone (Cay-13995). CGP 3466 dose-dependently increases survival of trophically withdrawn PC12 cells, decreases cytosine arabinoside-induced apoptosis of cerebellar granule cells, and increases the number of tyrosine hydroxylase-positive (TH+) mesencephalic dopaminergic neurons in vitro. Oral administration of CGP 3466 (0.14 mg/kg) increases the number of TH+ dopaminergic neurons in a rat model of Parkinson's disease induced by MPTP. It also reduces delayed acquisition in the Morris maze in a 6-OHDA-treated rat model of Parkinson's disease and increases survival in progressive motor neuronopathy (pmn) mice, a genetic model of amyotrophic lateral sclerosis (ALS). Formulations containing CGP 3466 are under clinical investigation for the treatment of Parkinson's disease and ALS.Formal Name: N-methyl-N-2-propyn-1-yl-dibenz[b,f]oxepin-10-methanamine, (2Z)-2-butenedioate. CAS Number: 200189-97-5. Synonyms: CGP 3466B. Molecular Formula: C19H17NO . C4H4O4. Formula Weight: 391.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 20 mg/ml, Ethanol: 0.5 mg/ml, PBS (pH 7.2): 0.5 mg/ml. lambdamax: 205, 282 nm. SMILES: CN(CC#C)CC1=CC2=CC=CC=C2OC3=C1C=CC=C3.OC(/C=C\C(O)=O)=O. InChi Code: InChI=1S/C19H17NO.C4H4O4/c1-3-12-20(2)14-16-13-15-8-4-6-10-18(15)21-19-11-7-5-9-17(16)19,5-3(6)1-2-4(7)8/h1,4-11,13H,12,14H2,2H3,1-2H,(H,5,6)(H,7,8)/b,2-1-. InChi Key: SQAZQLMBEHYFJA-BTJKTKAUSA-N.