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
Specifiche
Specifiche e purezza
≥98%
Meccanismi biochimici e fisiologici
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 i
Condizioni di conservazione di stoccaggio
Store at -20°C
Spedito in
Ice chest + Ice pads
Questo prodotto richiede spedizione a catena fredda. I servizi di terra e altri servizi economici non sono disponibili.
Tipo di azione
INHIBITOR
Purezza
≥98%
Nomi e identificatori
Peso molecolare
366.38
Dati avanzati
Certificati (CoA, COO, BSE/TSE e tabella di analisi)
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What is the purity of this product?
This product is supplied at ≥98% purity (chemical assay). Lot-specific values are stated on the Certificate of Analysis.
How should this product be stored?
Store at ?20 °C. Freezer storage is required to maintain the specified shelf life.
How is this product shipped?
This product ships in an insulated container with ice pads. Unpack on arrival and transfer it to the storage condition stated above.
What are the CAS number, molecular formula and molecular weight?
The CAS Number is 2765255-93-2, the molecular formula is C19H21F3N2O2, and the molecular weight is 366.38 g/mol.
What documentation is provided?
Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.
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