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Lu AF27139

Name: Lu AF27139
Brand: TargetMol
SKU: T9786
Price: 53 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T9786Cas No. 2097117-06-9

Lu AF27139 is an effective and selective antagonist of P2X7 receptor (IC50s of 12 and 2.4 nM for human and rat, Kis of 22, 54, and 13 nM for mouse, human, and rat, respectively). Lu AF27139 can be used in CNS diseases studies.

Lu AF27139

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Purity: 99.96%

Catalog No. T9786Cas No. 2097117-06-9

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$53	In Stock	In Stock
5 mg	$133	In Stock	In Stock
10 mg	$213	In Stock	In Stock
25 mg	$355	In Stock	In Stock
50 mg	$515	In Stock	In Stock
100 mg	$696	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$147	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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Purity:99.96%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	Lu AF27139 is an effective and selective antagonist of P2X7 receptor (IC50s of 12 and 2.4 nM for human and rat, Kis of 22, 54, and 13 nM for mouse, human, and rat, respectively). Lu AF27139 can be used in CNS diseases studies.
Targets&IC50	P2X7:12 nM (human), P2X7:2.4 nM (human), P2X7:22 nM (mouse), P2X7:54 nM (human)
In vitro	Lu AF27139 (100 nM) inhibits 300 μM BzATPinduced current in primary rat microglia with 80% inhibition occurring at a 100 nM dose. Lu AF27139 inhibits LPS-primed and BzATP-induced IL-1β release from THP-1 cells with an IC50 of 38 ± 2.5 nM. Lu AF27139 concentration-dependently blocks IL-1β release in rat and mouse primary cortical microglia primed with LPS and induces with 1 mM BzATP with IC50’s of 38 ± 19 nM in rat and 26 ± 6 nM in mice. Lu AF27139 (10-200 nM) inhibits 100 μM BzATP-induced current in HEK293 cells stably transfected with the rat P2X7R in a dose response manner with an IC50 of 66 nM[1].
In vivo	In male Sprague−Dawley rats and male C57BL mice, Lu AF27139 (p.o.; 3, 10, and 100 mg/kg) reduces intracerebroventricular administered LPS-primed and BzATP-triggered IL-1β release in the frontal cortex[1].

Chemical Properties

Molecular Weight	497.92
Formula	C₂₁H₁₉ClF₃N₅O₂S
Cas No.	2097117-06-9
Smiles	FC(F)(F)c1nc(sc1C(=O)NC[C@@H](N1CCOCC1)c1ccc(Cl)cc1)-c1ncccn1
Relative Density.	1.427 g/cm3 (Predicted)

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 120 mg/mL (241 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (8.03 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	2.0084 mL	10.0418 mL	20.0835 mL	100.4177 mL
5 mM	0.4017 mL	2.0084 mL	4.0167 mL	20.0835 mL
10 mM	0.2008 mL	1.0042 mL	2.0084 mL	10.0418 mL
20 mM	0.1004 mL	0.5021 mL	1.0042 mL	5.0209 mL
50 mM	0.0402 mL	0.2008 mL	0.4017 mL	2.0084 mL
100 mM	0.0201 mL	0.1004 mL	0.2008 mL	1.0042 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