A KAT II inhibitor (IC50s = 0.032 and 0.263 µM for human and rat recombinant enzymes

PF-04859989 (hydrochloride) – 5 mg

Brand:
Cayman
CAS:
177943-33-8
Storage:
-20
UN-No:
Non-Hazardous - /

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).{59036} 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.{59037}  

 

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SKU: 31383 - 5 mg Category:

Description

A KAT II inhibitor (IC50s = 0.032 and 0.263 µM for human and rat recombinant enzymes, respectively); selective for KAT II over KAT I, -III, and -IV (IC50s = 21.6, 107, and >50 µM, respectively); reduces basal striatum, prefrontal cortex, and hippocampus kynurenic acid levels in rats at 10 mg/kg; 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; inhibits GOT1 (IC50 = 8 µM); reduces the viability of PaTu 8988t and PaTu 8902 pancreatic cancer cells

Formal name: (3S)-3-amino-3,4-dihydro-1-hydroxy-2(1H)-quinolinone, monohydrochloride

Synonyms: 

Molecular weight: 214.7

CAS: 177943-33-8

Purity: ≥98%

Formulation: A solid

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