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首页-小分子抑制剂&激动剂-GPCR-GPR139-JNJ-3792165
JNJ-3792165

Chemical Structure : JNJ-3792165

CAS No.: 353504-63-9

JNJ-3792165 (JNJ3792165)

货号: PC-26127Not For Human Use, Lab Use Only.

JNJ-3792165 is a potent and selective antagonist at GPR139 with high affinity for human GPR139 (pKi =7.7, displacement of [3H] JNJ-6353054), behaves as an antagonist in [35S]GTPγS assay (pKb=7.4) and calcium mobilization assay.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

JNJ-3792165 is a potent and selective antagonist at GPR139 with high affinity for human GPR139 (pKi =7.7, displacement of [3H] JNJ-6353054), behaves as an antagonist in [35S]GTPγS assay (pKb=7.4) and calcium mobilization assay.
JNJ-3792165 displayed no significant affinity in a selectivity screen of over 50 other neurotransmitter and neuropeptide receptors at 1 uM.
JNJ-3792165 (10 uM) Completely blocks the effects of optogenetic stimulation of dynorphin release in dynorphinergic neurons of the nucleus accumbens at 10 uM.

物理化学性质&存储条件

分子量 374.27
分子式 C19H17Cl2N3O
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

1-(2,6-Dichlorobenzyl)-5-methyl-N-(m-tolyl)-1H-pyrazole-3-carboxamide

参考文献

1. Nepomuceno D, et al. Front Pharmacol 2018;9:157.

2. Xiaona Li, et al. Nat Commun. 2025 Jul 23;16(1):6786.

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