JNJ-28583113 is a potent and selective antagonist of the Transient Receptor Potential Melastatin 2 (TRPM2) ion channel, exhibiting an IC₅₀ of approximately 126 nM in human TRPM2 assays. This compound effectively inhibits TRPM2-mediated calcium influx, leading to the phosphorylation of GSK3α and GSK3β subunits. Functionally, JNJ-28583113 has demonstrated protective effects against oxidative stress-induced cell death and has been shown to suppress cytokine release in microglial cells in response to pro-inflammatory stimuli. Despite its efficacy and ability to penetrate the brain, its rapid in vivo metabolism limits its suitability for systemic dosing without further optimization
MedKoo Cat#: 128399
Name: JNJ-28583113
CAS#: 2765255-93-2
Chemical Formula: C19H21F3N2O2
Exact Mass: 366.1555
Molecular Weight: 366.38
Elemental Analysis: C, 62.29; H, 5.78; F, 15.56; N, 7.65; O, 8.73
The following data is based on the product molecular weight 366.38 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
