PF-04859989
PF-04859989 is a brain-penetrant, irreversible kynurenine aminotransferase (KAT) II inhibitor with IC50s of 23 and 263 nM for hKAT II and rKAT II. PF-04859989 is selective for KAT II over human KAT I, KAT III, and KAT IV (IC50s of 22, 11, and >50 μM, respectively) [1].
Product Specifications
CAS Number
34783-48-7
UNSPSC
12352005
Hazard Statement
H302-H315-H319-H332-H335
Target
Aminotransferases (Transaminases)
Type
Reference compound
Related Pathways
Metabolic Enzyme/Protease
Applications
Neuroscience-Neuromodulation
Field of Research
Neurological Disease
Assay Protocol
https://www.medchemexpress.com/pf-04859989.html
Smiles
O=C1N(O)C2=C(C=CC=C2)C[C@@H]1N
Molecular Formula
C9H10N2O2
Molecular Weight
178.19
Precautions
P261-P264-P270-P271-P280-P302+P352-P304+P340-P330-P362+P364-P405-P501
References & Citations
[1]"Amy B Dounay, et al. Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia. ACS Med Chem Lett . 2012 Jan 25;3 (3) :187-92."|[2]Linderholm KR, et al. Inhibition of kynurenine aminotransferase II reduces activity of midbrain dopamine neurons. Neuropharmacology. 2016;102:42-47.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
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