PF-04859989

Cat. No.: HY-113967: FAQs
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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).

For research use only. We do not sell to patients.

PF-04859989 Chemical Structure

CAS No. : 34783-48-7

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Other Forms of PF-04859989:

PF-04859989 hydrochloride Get quote

1 Publications Citing Use of MCE PF-04859989

•J Orthop Translat. 4 April 2022.

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Description

In Vivo

In vivo pharmacokinetic and efficacy studies in rat show that PF-04859989 is a brain-penetrant, irreversible inhibitor and is capable of reducing brain kynurenic acid by 50% at a dose of 10 mg/kg (sc)^[1].
Rats receiving PF-04859989 (5 mg/kg; i.p.) exhibited a significantly lower number of spontaneously active DA neurons pertrack^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Sprague-Dawley rats^[2]
Dosage:	5 mg/kg
Administration:	I.p.
Result:	Exhibited a significantly lower number of spontaneously active dopamine (DA) neurons pertrack compared to controls.

Molecular Weight

178.19

Formula

C₉H₁₀N₂O₂

CAS No.

34783-48-7

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[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." [Content Brief]

[2]. Linderholm KR, et al. Inhibition of kynurenine aminotransferase II reduces activity of midbrain dopamine neurons. Neuropharmacology. 2016;102:42-47. [Content Brief]

PF-04859989 Related Classifications

Neurological Disease

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PF-0485998934783-48-7PF04859989PF 04859989Othersmidbraindopamineneuronsschizophreniacognitive ,impairmentpsychiatricdisordersInhibitorinhibitorinhibit

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