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Chemical Structure : JNJ-28583113
Catalog No.: PC-72125Not For Human Use, Lab Use Only.
JNJ-28583113 (JNJ28583113) is a potent, selective, brain penetrant TRPM2 antagonist with IC50 of 126 nM (hTRPM2).
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JNJ-28583113 (JNJ28583113) is 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.
| M.Wt | 366.384 | |
| Formula | C19H21F3N2O2 | |
| Appearance | Solid | |
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1. Lawrence Fourgeaud, et al. Eur J Pharmacol. 2019 Jun 15;853:299-307.
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