PF-04859989 (hydrochloride)

PF-04859989 is an inhibitor of kynurenine aminotransferase II (KAT II, IC50s = 0.032 and 0.263 µM for human and rat recombinant enzymes, respectively). It is selective for KAT II over KAT I, -III, and -IV (IC50s = 21.6, 107, and >50 µM, respectively). In vivo, PF-04859989 (10 mg/kg, s.c.) reduces basal striatum, prefrontal cortex, and hippocampus kynurenic acid levels in rats. It prevents ketamine- or amphetamine-induced disruption of auditory gating in rats, as well as prevents ketamine-induced deficits in spatial memory in non-human primates. PF-04859989 also inhibits glutamate oxaloacetate transaminase 1 (GOT1, IC50 = 8 µM) and reduces the viability of PaTu 8988t and PaTu 8902 pancreatic cancer cells in a concentration-dependent manner.Formal Name: (3S)-3-amino-3,4-dihydro-1-hydroxy-2(1H)-quinolinone, monohydrochloride. CAS Number: 177943-33-8. Molecular Formula: C9H10N2O2 . HCl. Formula Weight: 214.7. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: 22 mg/ml, Water: 22 mg/ml. SMILES: ON1C2=CC=CC=C2C[C@@H](C1=O)N.Cl. InChi Code: InChI=1S/C9H10N2O2.ClH/c10-7-5-6-3-1-2-4-8(6)11(13)9(7)12,/h1-4,7,13H,5,10H2,1H/t7-,/m0./s1. InChi Key: WZOBDOKCHIUXAY-FJXQXJEOSA-N.