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PF-04859989 HCl

Name: PF-04859989 HCl
Brand: TargetMol
SKU: T28368
Price: 38 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T28368Cas No. 177943-33-8

Alias PF-04859989HCl, PF-04859989, PF04859989, PF 04859989

PF-04859989 HCl is a brain-penetrable and irreversible inhibitor of kynurenine amino transferase II (KAT II), which is the enzyme responsible for most of the brain synthesis of kynurenic acid.

PF-04859989 HCl

🥰Excellent

Purity: 98.31%

Catalog No. T28368Alias PF-04859989HCl, PF-04859989, PF04859989, PF 04859989Cas No. 177943-33-8

PF-04859989 HCl is a brain-penetrable and irreversible inhibitor of kynurenine amino transferase II (KAT II), which is the enzyme responsible for most of the brain synthesis of kynurenic acid.

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$38	In Stock	In Stock
5 mg	$60	In Stock	In Stock
10 mg	$98	In Stock	In Stock
25 mg	$189	In Stock	In Stock
50 mg	$297	In Stock	In Stock
100 mg	$488	In Stock	In Stock
200 mg	$682	In Stock	In Stock
500 mg	$1,060	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$66	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:98.31%

Appearance:Solid

Color:White

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COA

Product Introduction

Bioactivity

Description	PF-04859989 HCl is a brain-penetrable and irreversible inhibitor of kynurenine amino transferase II (KAT II), which is the enzyme responsible for most of the brain synthesis of kynurenic acid.
Targets&IC50	KAT II:23 nM(human), KAT II:263 nM(rat), KAT I:22 μM, KAT IV:>50 μM, KAT III:11 μM
In vitro	The IC50s values are 23 and 263 nM for hKAT II and rKAT II. PF-04859989 HCl is selective for KAT II over human KAT I, KAT III, and KAT IV (IC50s of 22, 11, and >50 μM, respectively)[3].
In vivo	Acute administration of the KAT II inhibitor PF-04859989 (5 or 10 mg/kg) was associated with a short-onset, time-dependent decrease in firing rate and burst activity of DA neurons, both parameters reaching a 50% reduction within 45 min. Furthermore, PF-04859989 reduced the number of spontaneously active DA cells as measured 4-6 after administration. Pretreatment with d-cycloserine (30 mg/kg) or CGP-52432 (10 mg/kg) prevented the inhibitory action of PF-04859989 (5 mg/kg) on firing rate and burst firing activity. In contrast, pretreatment with methyllycaconitine (MLA, 4 mg/kg) did not change the response, whereas picrotoxin (4.5 mg/kg) partially prevented the inhibitory effects of PF-04859989 (5 mg/kg, i.v.)[2].
Synonyms	PF-04859989HCl, PF-04859989, PF04859989, PF 04859989

Chemical Properties

Molecular Weight	214.65
Formula	C₉H₁₁ClN₂O₂
Cas No.	177943-33-8
Smiles	Cl.N[C@H]1Cc2ccccc2N(O)C1=O
Relative Density.	1.31g/cm3

Storage & Solubility Information

Storage

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 100 mg/mL (465.87 mM), Sonication is recommended.

H2O: 100 mg/mL (465.87 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (18.63 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO/H2O

	1mg	5mg	10mg	50mg
1 mM	4.6587 mL	23.2937 mL	46.5875 mL	232.9373 mL
5 mM	0.9317 mL	4.6587 mL	9.3175 mL	46.5875 mL
10 mM	0.4659 mL	2.3294 mL	4.6587 mL	23.2937 mL
20 mM	0.2329 mL	1.1647 mL	2.3294 mL	11.6469 mL
50 mM	0.0932 mL	0.4659 mL	0.9317 mL	4.6587 mL
100 mM	0.0466 mL	0.2329 mL	0.4659 mL	2.3294 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc