JNJ-42253432 | P2X7 antagonist | Probechem Biochemicals

Chemical Structure : JNJ-42253432

CAS No.: 1428327-35-8

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JNJ-42253432 (JNJ 42253432, JNJ42253432)

货号: 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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10 mg	￥7280	In stock
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生物&药学活性

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.

物理化学性质&存储条件

分子量	446.639
分子式	C28H38N4O
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
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

参考文献

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.

JNJ-42253432 (JNJ 42253432, JNJ42253432)

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JNJ-42253432 (JNJ 42253432, JNJ42253432)

生物&药学活性

物理化学性质&存储条件

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