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Referencia número: HY-113967

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PF-04859989

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

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).

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No. CAS: 34783-48-7
Fòrmula: C₉H₁₀N₂O₂
Peso molecular:178.19

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

Data Sheet (274 KB)

PF-04859989 Chemical Structure

No. CAS: 34783-48-7

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

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Descripciòn

Ver todos los productos específicos de isoformas Aminotransferases (Transaminases) :

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.

Chemical Information

No. CAS 34783-48-7
Peso molecular 178.19
Fòrmula C₉H₁₀N₂O₂
SMILES

O=C1N(O)C2=C(C=CC=C2)C[C@@H]1N
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

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

Publications (1)

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J Orthop Translat

Exercised accelerated the production of muscle-derived kynurenic acid in skeletal muscle and alleviated the postmenopausal osteoporosis through the Gpr35/NFκB p65 pathway. [Abstract]

2022 Apr 4:35:1-12. PMID: 35846727

Pureza y Documentación

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Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (274 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[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]

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1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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PF-04859989

1 Cited Publications

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PF-04859989

Publications Citing Use of MedChemExpress (MCE) PF-04859989

Ver todos los productos específicos de isoformas Aminotransferases (Transaminases)

Actividad biológica

Chemical Information

Publications (1)

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