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PZ0250

Sigma-Aldrich

PF-04859989 hydrochloride

≥98% (HPLC)

Synonym(s):

(3S)-3-Amino-1-hydroxy-3,4-dihydroquinolin-2(1H)-one; L-3-Amino-3,4-dihydro-1-hydroxycarbstyril hydrochloride, PF-4859989 hydrochloride, PF04859989 hydrochloride

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About This Item

Empirical Formula (Hill Notation):
C9H10N2O2 · HCl
CAS Number:
177943-33-8
Molecular Weight:
214.65
MDL number:
MFCD22419400
UNSPSC Code:
51111800
PubChem Substance ID:
329823792
NACRES:
NA.77

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

H2O: 20 mg/mL, clear

storage temp.

room temp

SMILES string

N[C@H]1CC2=CC=CC=C2N(O)C1=O.Cl

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

Biochem/physiol Actions

PF-04859989 is a brain-penetrable irreversible inhibitor of kynurenine amino transferase II (KAT II), the enzyme responsible for most of the brain synthesis of kynurenic acid, which has been implicated in several psychiatric and neurological disorders, including schizophrenia and bipolar disorder, and thought to impair cognitive function. PF-04859989 has IC50 values of 23 nM for hKAT II and 263 nM for rKAT II. PF-04859989 is ~1000-fold selective for KAT II over human KAT I, KAT III, and KAT IV. PF-04859989 prevented ketamine-induced disruption of performance in memory tasks in both rodents and nonhuman primates.

Features and Benefits

This compound is a featured product for Neuroscience research. Click here to discover more featured Neuroscience products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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George Zakhary et al.
Journal of neuroscience research, 98(1), 155-167 (2019-07-02)
Neurosurgical procedures result in surgically induced brain injury (SBI) that causes postoperative complications including brain edema and neuronal apoptosis in the surrounding brain tissue. SBI leads to the release of cytokines that indirectly cause the stimulation of kynurenine 3-monooxygenase (KMO)

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