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PF-04859989 hydrochloride 

Cat. No.: HY-116451
Handling Instructions

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).

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

PF-04859989 hydrochloride Chemical Structure

PF-04859989 hydrochloride Chemical Structure

CAS No. : 177943-33-8

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Description

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].

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].

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

214.65

Formula

C₉H₁₁ClN₂O₂

CAS No.

177943-33-8

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

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Keywords:

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PF-04859989 hydrochloride
Cat. No.:
HY-116451
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