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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 (human):126 nM, TRPM2 (rat):25 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 |
| Color | White |
| Appearance | Solid |
| 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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