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JNJ-42253432

Chemical Structure : JNJ-42253432

CAS No.: 1428327-35-8

JNJ-42253432 (JNJ 42253432, JNJ42253432)

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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 446.639
Formula C28H38N4O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-methyl-N-([1-(4-phenylpiperazin-1-yl)cyclohexyl]methyl)-1,2,3,4-tetrahydroisoquinoline-5-carboxamide

References

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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