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GSK-1482160

Name: GSK-1482160
Brand: TargetMol
SKU: T61025
Price: 30 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T61025Cas No. 1001389-72-5

GSK-1482160 is a CNS-penetrant negative allosteric modulator of P2X7 receptor with oral activity. The P2X7 receptor is involved in the production of pro-inflammatory cytokines by central and peripheral immune cells, so GSK-1482160 has the potential to study inflammatory diseases. GSK-1482160 shows excellent in vitro potency (in functional and electrophysiological assays at recombinant and naive P2X7 receptors across multiple species including humans) and cross-target selectivity.

GSK-1482160

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Purity: 99.57%

Catalog No. T61025Cas No. 1001389-72-5

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$30	In Stock	In Stock
10 mg	$46	In Stock	In Stock
25 mg	$94	In Stock	In Stock
50 mg	$166	In Stock	In Stock
100 mg	$245	-	In Stock
1 mL x 10 mM (in DMSO)	$32	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:99.57%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	GSK-1482160 is a CNS-penetrant negative allosteric modulator of P2X7 receptor with oral activity. The P2X7 receptor is involved in the production of pro-inflammatory cytokines by central and peripheral immune cells, so GSK-1482160 has the potential to study inflammatory diseases. GSK-1482160 shows excellent in vitro potency (in functional and electrophysiological assays at recombinant and naive P2X7 receptors across multiple species including humans) and cross-target selectivity.
In vitro	ATP-induced secretion of tau-containing exosome was significantly suppressed by GSK-1482160 treatment from primary murine microglia, but not from neurons or astrocytes [2].
In vivo	Oral administration of GSK-1482160 significantly reduced accumulation of MC1+ and Alz50+ misfolded tau in hippocampal regions, which was accompanied with reduced accumulation of Tsg101, an exosome marker, in hippocampal neurons. GSK-1482160 also significantly increased accumulation of Tsg101 and CD81 in microglia in vivo, suggesting its suppression of P2RX7-induced exosome secretion from microglia [2].

Chemical Properties

Molecular Weight	334.72
Formula	C₁₄H₁₄ClF₃N₂O₂
Cas No.	1001389-72-5
Smiles	CN1[C@@H](CCC1=O)C(=O)NCc1cccc(c1Cl)C(F)(F)F

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 90 mg/mL (268.88 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.9876 mL	14.9379 mL	29.8757 mL	149.3786 mL
5 mM	0.5975 mL	2.9876 mL	5.9751 mL	29.8757 mL
10 mM	0.2988 mL	1.4938 mL	2.9876 mL	14.9379 mL
20 mM	0.1494 mL	0.7469 mL	1.4938 mL	7.4689 mL
50 mM	0.0598 mL	0.2988 mL	0.5975 mL	2.9876 mL
100 mM	0.0299 mL	0.1494 mL	0.2988 mL	1.4938 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