JNJ-28583113
Based on 5 publication(s) in Google Scholar
JNJ-28583113 is an TRPM2 antagonist with brain permeability. JNJ-28583113 inhibits TRPM2 blocked phosphorylation of GSK3α and β subunits. JNJ-28583113 protects cells from oxidative stress induced cell death. JNJ-28583113 also suppresses cytokine release in response to pro-inflammatory stimuli in microglia.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.82%
- CAS. Nr.: 2765255-93-2
- Formel: C19H21F3N2O2
- Molecular Weight:366.38
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) JNJ-28583113
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Biologische Aktivität
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TRPM2 |
JNJ-28583113 inhibits TRPM2 in cells overexpressing chimpanzee (IC50=100 nM), rat (IC50=25 nM), and human (IC50=126 nM), respectively[1].
JNJ-28583113 (3 nM, 30 nM, and 1 μM; 200 s) exhibits electrophysical characterization in ADPR-induced currents recorded in hTRPM2-HEK-inducible cells[1].
JNJ-28583113 (10 μM; 1 h) prevents cells from H2O2 induced cell death up to 1 mM of H2O2. JNJ-28583113 (10 μM; 1 h) also protects HeLa cells from H2O2 (10 μM; 1 h) induced morphological changes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:hTRPM2-HEK cells
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Concentration:10 μM
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Incubation Time:30 min
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Result:Recovered phosphorylation of GSK3α and β subunits which inhibited by H2O2 (300 μM; 10 min).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Harlan Sprague Dawley Rats (400 g)[1]
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Dosage:10 mg/kg, 2 mL/kg
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Administration:SC; sampled at 0.5, 2, or 6 h post dosing
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Result:Quickly metabolized in the plasma, while it showed high levels in plasma and low levels in the brain.
Chemical Information
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CAS. Nr. 2765255-93-2
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Appearance Solid
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Molecular Weight 366.38
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Formel C19H21F3N2O2
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Color White to off-white
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SMILES
O=C(CN1N=C(C2=C1CCCCC2)C3=CC=C(C(F)(F)F)C=C3)OCC
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (5)
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Journal Impact Factor
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Most Recent
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Nat Immunol
Lipid asymmetry disruption by XKR8 orchestrates neutrophil extracellular trap formation and inhibits fungal infection. [Abstract]2026 May;27(5):949-960. PMID: 41781710 -
Adv Sci (Weinh)
Targeting Transient Receptor Potential Melastatin-2 (TRPM2) Enhances Therapeutic Efficacy of Third Generation EGFR Inhibitors against EGFR Mutant Lung Cancer. [Abstract]2024 Sep;11(35):e2310126. PMID: 39044361 -
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Free Radic Biol Med
Nano-selenium alleviates cadmium-induced ferroptosis in chicken liver by modulating the TRPM2 channel. [Abstract]2026 Jan:242:495-507. PMID: 41197751 -
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (272.94 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7294 mL | 13.6470 mL | 27.2941 mL | 68.2352 mL |
| 5 mM | 0.5459 mL | 2.7294 mL | 5.4588 mL | 13.6470 mL | |
| 10 mM | 0.2729 mL | 1.3647 mL | 2.7294 mL | 6.8235 mL | |
| 15 mM | 0.1820 mL | 0.9098 mL | 1.8196 mL | 4.5490 mL | |
| 20 mM | 0.1365 mL | 0.6824 mL | 1.3647 mL | 3.4118 mL | |
| 25 mM | 0.1092 mL | 0.5459 mL | 1.0918 mL | 2.7294 mL | |
| 30 mM | 0.0910 mL | 0.4549 mL | 0.9098 mL | 2.2745 mL | |
| 40 mM | 0.0682 mL | 0.3412 mL | 0.6824 mL | 1.7059 mL | |
| 50 mM | 0.0546 mL | 0.2729 mL | 0.5459 mL | 1.3647 mL | |
| 60 mM | 0.0455 mL | 0.2275 mL | 0.4549 mL | 1.1373 mL | |
| 80 mM | 0.0341 mL | 0.1706 mL | 0.3412 mL | 0.8529 mL | |
| 100 mM | 0.0273 mL | 0.1365 mL | 0.2729 mL | 0.6824 mL |
JNJ-28583113 Related Classifications
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