| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C19H21F3N2O2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
JNJ-28583113 is a brain-permeable antagonist of TRPM2. TRPM2 inhibition blocks phosphorylation of the GSK3α and GSK3β subunits, protects cells from oxidative-stress-induced cell death, and suppresses cytokine release from microglia in response to pro-inflammatory stimuli[1]. It is supplied as a white to off-white solid (C19H21F3N2O2, MW 366.38) at 98.82% purity.
Physical & Chemical Properties
| CAS Number | 2765255-93-2 |
|---|---|
| Molecular Formula | C19H21F3N2O2 |
| Molecular Weight | 366.38 g/mol |
| Purity | 98.82% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | O=C(CN1N=C(C2=C1CCCCC2)C3=CC=C(C(F)(F)F)C=C3)OCC |
| Target | TRPM2 |
| Signaling Pathway | Membrane Transporter/Ion Channel; Neuronal Signaling |
| Solubility | In Vitro: DMSO: 100 mg/mL (272.94 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 100 mg/mL (272.94 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 2% DMSO + 40% PEG300 + 5% Tween-80 + 53% saline |
|---|---|
| Result | ≥ 2 mg/mL (5.46 mM); clear solution |
Protocol 2
| Composition | 2% DMSO + 98% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2 mg/mL (5.46 mM); clear solution |
Data provided by the manufacturer.
In Vitro
TRPM2 inhibition by JNJ-28583113 gives IC50=100 nM for chimpanzee, IC50=25 nM for rat, and IC50=126 nM for human, in cells overexpressing the channel[1]. In hTRPM2-HEK-inducible cells, JNJ-28583113 (3 nM, 30 nM, and 1 μM; 200 s) shows electrophysical characterization of ADPR-induced currents[1]. JNJ-28583113 (10 μM; 1 h) protects cells against H2O2-induced cell death at H2O2 concentrations up to 1 mM. JNJ-28583113 (10 μM; 1 h) also protects HeLa cells from morphological changes induced by H2O2 (10 μM; 1 h)[1].
Western Blot Analysis[1]
| Cell Line | hTRPM2-HEK cells |
|---|---|
| Concentration | 10 μM |
| Incubation Time | 30 min |
| Result | Recovered phosphorylation of GSK3α and β subunits which inhibited by H2O2 (300 μM; 10 min). |
In Vivo
Brain penetration is shown by JNJ-28583113 (10 mg/kg, 2 ml/kg; sc; single dose), which reaches 400 ng/mL in the brain compartment[1].
| Animal Model | Harlan Sprague Dawley Rats (400 g)[1] |
|---|---|
| Dosage | 10 mg/kg, 2 mL/kg |
| Administration | SC; sampled at 0.5, 2, or 6 h post dosing |
| Result | Quickly metabolized in the plasma, while it showed high levels in plasma and low levels in the brain. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Lipid asymmetry disruption by XKR8 orchestrates neutrophil extracellular trap formation and inhibits fungal infection. Nat Immunol 2026 May;27(5):949-960. PMID: 41781710
Targeting Transient Receptor Potential Melastatin-2 (TRPM2) Enhances Therapeutic Efficacy of Third Generation EGFR Inhibitors against EGFR Mutant Lung Cancer. Adv Sci (Weinh) 2024 Sep;11(35):e2310126. PMID: 39044361
Chem Eng J. 2026 Feb 5.
Nano-selenium alleviates cadmium-induced ferroptosis in chicken liver by modulating the TRPM2 channel. Free Radic Biol Med 2026 Jan:242:495-507. PMID: 41197751
bioRxiv. 2025 Feb 16.
