JNJ-28583113

SKU: orb3032920

Description

JNJ-28583113 (JNJ28583113) a potent, selective, brain penetrant TRPM2 antagonist with IC50 of 126 nM (hTRPM2).JNJ-28583113 shows similar potency against species chimpanzee and rat TRPM2 with IC50 of 100 and 25 nM, respectively.JNJ-28583113 shows no significant (IC50>10 uM) reactivity towards PARP or PARG and a panel for multiple known kinases GPCRs and ion channels, nine other TRP channels with exception of TRPM5 (IC50<1 uM).Blocking TRPM2 via JNJ-28583113 caused phosphorylation of GSK3α and β subunits in cell assays.JNJ-28583113 also protected cells from oxidative stress induced cell death as well as morphological changes induced by non-cytotoxic concentrations of H2O2。JNJ-28583113 blunted cytokine release in response to pro-inflammatory stimuli in microglia.JNJ-28583113 was brain penetrant but not suitable for systemic dosing as it was rapidly metabolized in vivo, but the in-vitro pharmacology of JNJ-28583113 is the best in class.

Key Properties

• CAS Number: 2765255-93-2
• MW: 366.377455472946
• Purity: 0.98
• Formula: C₁₉H₂₁F₃N₂O₂
• SMILES: N1=C(C2=CC=C(C(F)(F)F)C=C2)C2CCCCCC=2N1CC(OCC)=O

Storage & Handling

• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only