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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-iGluR-JNJ-78911118
JNJ-78911118

Chemical Structure : JNJ-78911118

CAS No.:

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JNJ-78911118 (JNJ 78911118)

货号: PC-24631Not For Human Use, Lab Use Only.

JNJ-78911118 is a potent, centrally-penetrant, selective antagonist of GluN2A-containing NMDA receptors, blocks GluN1/2AR-induced calcium flux with IC50 of 46 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

JNJ-78911118 is a potent, centrally-penetrant, selective antagonist of GluN2A-containing NMDA receptors, blocks GluN1/2AR-induced calcium flux with IC50 of 46 nM.
JNJ-78911118 acts selectively as a negative allosteric modulator of both di- and triheteromeric GluN2A receptors.
JNJ-78911118 shows no activity against GluN1/2B and GluN1/2C receptors and no meaningful activity or GluN1/2D receptors.
JNJ-78911118 binds to the GluN1/2A interface and is a NAM of glycine activity.
JNJ-78911118 produces dose-dependent exposures in plasma and brain, as well as dose-dependent hippocampal receptor occupancy in rats.
JNJ-78911118 produced concentration-dependent receptor occupancy, increased prefrontal cortex monoamine levels in wild type, but not in GluN2A knockout mice, and blocked theta burst induced LTP in the hippocampus.
JNJ-78911118 produced increases in dendritic complexity and synapse number in vitro, and increased mEPSC frequency in rat cortical neurons in vivo.

物理化学性质&存储条件

分子量 419.82
分子式 C19H16ClF2N5O2
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

5-(2-(4-chloropyridin-2-yl)-2,2-difluoroethoxy)-6-methyl-N-(pyridin-3-ylmethyl)pyrazine-2-carboxamide

参考文献

1. Lord B, et al. Br J Pharmacol. 2025 May 13. doi: 10.1111/bph.70069.

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