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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 Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $84 | In Stock | In Stock | |
| 5 mg | $198 | In Stock | In Stock | |
| 10 mg | $247 | In Stock | In Stock | |
| 25 mg | $397 | In Stock | In Stock | |
| 50 mg | $616 | In Stock | In Stock | |
| 100 mg | $786 | - | In Stock | |
| 200 mg | $1,090 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $218 | In Stock | In Stock |
| 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] |
| Synonyms | JNJ28583113 |
| Molecular Weight | 366.38 |
| Formula | C19H21F3N2O2 |
| Cas No. | 2765255-93-2 |
| Smiles | O=C(OCC)CN1N=C(C=2C=CC(=CC2)C(F)(F)F)C3=C1CCCCC3 |
| 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: 80 mg/mL (218.35 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
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.
1) Add 100 μL of the DMSO
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
and mix thoroughly until a homogeneous solution is obtained.
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