JNJ-28583113

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 In Vitro JNJ-28583113 inhibits TRPM2 in cells overexpressing chimpanzee (IC 50 =100 nM), rat (IC 50 =25 nM), and human (IC 50 =126 nM), respectively. JNJ-28583113 (3 nM, 30 nM, and 1 μM; 200 s) exhibits electrophysical characterization in ADPR-induced currents recorded in hTRPM2-HEK-inducible cells. JNJ-28583113 (10 μM; 1 h) prevents cells from H 2 O 2 induced cell death up to 1 mM of H 2 O 2 . JNJ-28583113 (10 μM; 1 h) also protects HeLa cells from H 2 O 2 (10 μM; 1 h) induced morphological changes. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: hTRPM2-HEK cells Concentration: 10 μM Incubation Time: 30 min Result: Recovered phosphorylation of GSK3α and β subunits which inhibited by H 2 O 2 (300 μM; 10 min). In Vivo JNJ-28583113 (10 mg/kg, 2 ml/kg; sc; single dose) is brain penetrant, and achieves 400 ng/mL in the brain compartment . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Harlan Sprague Dawley Rats (400 g) 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. Form:Solid IC50& Target:TRPM2

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