Products for Research Use Only

JNJ-28583113

CAT: 0013-GTR19259609-01Size: 100 mgDry Ice: NoHazardous: No
Product image 1
1 / 1
CAT#:0013-GTR19259609-01Size:100 mg
Selected
24/48H Stock Items & 2 to 6 Weeks non Stock Items.
Quick Request Actions
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.
CAS Number
2765255-93-2
Purity
0.98
Smiles
N1=C (C2=CC=C (C (F) (F) F) C=C2) C2CCCCCC=2N1CC (OCC) =O
Molecular Formula
C19H21F3N2O2
Molecular Weight
366.377455472946
Notes
For research use only.