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PF-05180999

Name: PF-05180999
Brand: TargetMol
SKU: T16484
Price: 40 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T16484Cas No. 1394033-54-5

Alias PF-999, PF999, PF-5180999, PF5180999, PF05180999

PF-05180999 (PF-999) is a selective and potent phosphodiesterase 2A (PDE2A) inhibitor that enhances long-term memory in a contextual fear conditioned reflex model in rats.

PF-05180999

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Purity: 99.82%

Catalog No. T16484Alias PF-999, PF999, PF-5180999, PF5180999, PF05180999Cas No. 1394033-54-5

PF-05180999 (PF-999) is a selective and potent phosphodiesterase 2A (PDE2A) inhibitor that enhances long-term memory in a contextual fear conditioned reflex model in rats.

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$40	-	In Stock
5 mg	$64	-	In Stock
10 mg	$113	-	In Stock
25 mg	$239	-	In Stock
50 mg	$396	-	In Stock
100 mg	$691	-	In Stock
1 mL x 10 mM (in DMSO)	$71	-	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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Purity:99.82%

Appearance:Solid

Color:White to Yellow

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	PF-05180999 (PF-999) is a selective and potent phosphodiesterase 2A (PDE2A) inhibitor that enhances long-term memory in a contextual fear conditioned reflex model in rats.
Targets&IC50	PDE2A (monkey):5.5 nM (Ki), PDE2A (dog):8.4 nM (Ki), PDE10A1:2.03 μM, PDE2A (rat):4.2 nM (Ki), PDE7B:26.969 μM, PDE2A (dog):5.2 nM, PDE11A4:50.09 μM, PDE2A (rat):2.6 nM, PDE2A (monkey):3.4 nM
In vitro	PF-05180999 is a weak inducer of CYP3A4 with no direct inhibition of human recombinant cytochrome P450 enzymes (including 1A2, 2B6, 2C8, 2C9, 2C19, 2D6, and 3A) and does not induce CYP1A2.PF-05180999 binds to PDE2A in rat, dog, and monkey with Ki values of 4.2 nM 8.4 nM, and 5.5 nM, with IC50 values of 2.6 nM, 5.2 nM, and 3.4 nM, respectively.For the other PDE isoforms, PF-05180999 was weakly active, with IC50s of 2.03 μM (PDE10A1), 26.969 μM (PDE7B), 50.09 μM (PDE11A4), and >56.25 μM (PDE1B1, PDE3A1, PDE4D3, PDE5A1, PDE6 (bovine), PDE8B, PDE9A1). [1]
In vivo	PF-05180999 induced an acute, dose-dependent increase in cGMP levels in mouse cortex, striatum and hippocampus, but had no effect on cAMP levels and its downstream phosphorylated cAMP response element binding protein (p-CREB). In the radial arm maze (RAM) model of working memory, subcutaneous injection of 0.032-0.32 mg/kg PF-05180999 significantly reduced ketamine-induced working memory errors in rats. [1]
Synonyms	PF-999, PF999, PF-5180999, PF5180999, PF05180999

Chemical Properties

Molecular Weight	414.39
Formula	C₁₉H₁₇F₃N₈
Cas No.	1394033-54-5
Smiles	FC(F)(F)C=1C=NC(=CC1)C2=C(C=NN2C)C=3N=C(N4N=CN=C(C34)N5CCC5)C
Relative Density.	1.57 g/cm3 (Predicted)

Storage & Solubility Information

Storage

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 40 mg/mL (96.53 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.83 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

	1mg	5mg	10mg	50mg
1 mM	2.4132 mL	12.0659 mL	24.1319 mL	120.6593 mL
5 mM	0.4826 mL	2.4132 mL	4.8264 mL	24.1319 mL
10 mM	0.2413 mL	1.2066 mL	2.4132 mL	12.0659 mL
20 mM	0.1207 mL	0.6033 mL	1.2066 mL	6.0330 mL
50 mM	0.0483 mL	0.2413 mL	0.4826 mL	2.4132 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