PF-04859989 (hydrochloride)

PF-04859989 hydrochloride 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 hydrochloride 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

[177943-33-8]

Product Name Alternative

UR-8880

UNSPSC

12352005

Hazard Statement

H315, H319, H320

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-hydrochloride.html

Purity

99.90

Solubility

DMSO : 20.83 mg/mL (ultrasonic; warming; heat to 60°C) |H2O : 100 mg/mL (ultrasonic)

Smiles

O=C1N(O)C2=C(C=CC=C2)C[C@@H]1N.[H]Cl

Molecular Formula

C9H11ClN2O2

Molecular Weight

214.65

Precautions

H315, H319, H320

References & Citations

[1]Dounay AB, et al. Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia. ACS Med Chem Lett. 2012;3 (3) :187-192. Published 2012 Jan 25.|[2]Linderholm KR, et al. Inhibition of kynurenine aminotransferase II reduces activity of midbrain dopamine neurons. Neuropharmacology. 2016;102:42-47.