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JNJ-28583113

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Catalog No. T74779Cas No. 2765255-93-2
Alias JNJ28583113

JNJ-28583113 is a brain-penetrant TRPM2 antagonist that induces phosphorylation of GSK3α and β subunits, protecting cells from oxidative stress-induced cell death. It inhibits microglia response to pro-inflammatory stimuli, used in the study of neurological diseases.

JNJ-28583113

JNJ-28583113

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Purity: 98.57%
Catalog No. T74779Alias JNJ28583113Cas No. 2765255-93-2
JNJ-28583113 is a brain-penetrant TRPM2 antagonist that induces phosphorylation of GSK3α and β subunits, protecting cells from oxidative stress-induced cell death. It inhibits microglia response to pro-inflammatory stimuli, used in the study of neurological diseases.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$84In StockIn Stock
5 mg$198In StockIn Stock
10 mg$247In StockIn Stock
25 mg$397In StockIn Stock
50 mg$616In StockIn Stock
100 mg$786-In Stock
200 mg$1,090-In Stock
1 mL x 10 mM (in DMSO)$218In StockIn 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:98.57%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
JNJ-28583113 is a brain-penetrant TRPM2 antagonist that induces phosphorylation of GSK3α and β subunits, protecting cells from oxidative stress-induced cell death. It inhibits microglia response to pro-inflammatory stimuli, used in the study of neurological diseases.
Targets&IC50
TRPM2 (rat):25 nM, TRPM2 (human):126 nM
In vitro
JNJ-28583113 is a potent TRPM2 antagonist, blocking TRPM2 leads to phosphorylation of GSK3α and β subunits. JNJ-28583113 blocks TRPM2 in chimpanzees, rats, and humans with IC50 values of 100 nM, 25 nM, and 126 nM, respectively. [1]
In vivo
JNJ-28583113 (10 mg/kg, injected subcutaneously) is brain permeable, reaches 400 ng/ml in the brain compartment, and is rapidly metabolized in plasma. [1]
SynonymsJNJ28583113
Chemical Properties
Molecular Weight366.38
FormulaC19H21F3N2O2
Cas No.2765255-93-2
SmilesO=C(OCC)CN1N=C(C=2C=CC(=CC2)C(F)(F)F)C3=C1CCCCC3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 80 mg/mL (218.35 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.7294 mL13.6470 mL27.2941 mL136.4703 mL
5 mM0.5459 mL2.7294 mL5.4588 mL27.2941 mL
10 mM0.2729 mL1.3647 mL2.7294 mL13.6470 mL
20 mM0.1365 mL0.6824 mL1.3647 mL6.8235 mL
50 mM0.0546 mL0.2729 mL0.5459 mL2.7294 mL
100 mM0.0273 mL0.1365 mL0.2729 mL1.3647 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:
TargetMol | Animal experiments 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 DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | 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.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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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
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