Chemical Structure : JNJ-42253432
CAS No.: 1428327-35-8
Catalog No.: PC-60767Not For Human Use, Lab Use Only.
JNJ-42253432 is a potent, selective, CNS-penetrant P2X7 antagonist with pKi of 9.1 and 7.9 for rat and huamn P2X7 channel, respectively.
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JNJ-42253432 is a potent, selective, CNS-penetrant P2X7 antagonist with pKi of 9.1 and 7.9 for rat and huamn P2X7 channel, respectively.
JNJ-42253432 does not block calcium flux via human P2X1, P2X2, P2X3, P2X2/P2X3, and P2X4 at 10 uM.
JNJ-42253432 attenuates both ATP- and Bz-ATP-induced currents from hP2X7-1321N1 cells with similar potencies (pEC50=7.0).
JNJ-42253432 blocks the release of IL-1β induced by Bz-ATP in freely moving rat brain, also increases serotonin levels.
JNJ-42253432 attenuates amphetamine-induced hyperactivity in vivo.
M.Wt | 446.639 | |
Formula | C28H38N4O | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
2-methyl-N-([1-(4-phenylpiperazin-1-yl)cyclohexyl]methyl)-1,2,3,4-tetrahydroisoquinoline-5-carboxamide |
1. Lord B, et al. J Pharmacol Exp Ther. 2014 Dec;351(3):628-41.
2. Amhaoul H, et al. Neuropharmacology. 2016 Jun;105:175-185.
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