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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 | Availability | Quantity |
---|---|---|---|
1 mg | $87 | In Stock | |
5 mg | $209 | In Stock | |
10 mg | $312 | In Stock | |
25 mg | $488 | In Stock | |
50 mg | $846 | In Stock | |
100 mg | $1,460 | In Stock | |
200 mg | $1,970 | In Stock | |
1 mL x 10 mM (in DMSO) | $218 | 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] |
Alias | 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 | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 80 mg/mL (218.35 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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