JNJ-63533054,1802326-66-4

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产品名称：JNJ-63533054

产品别名：JNJ 63533054,JNJ63533054

英文别名：JNJ 63533054;JNJ63533054

靶点：GPR139

CAS：1802326-66-4

纯度：>98%

外观：Powder

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：JNJ-63533054 is a potent and selective agonist of hGPR139 with an EC50 = 16 nM.

溶解性：10 mM in DMSO

体外研究：

JNJ-63533054 specifically activates human GPR139 in the calcium mobilization (EC50 = 16 ± 6 nM) and GTPγS binding (EC50 = 17 ± 4 nM) assays. JNJ-63533054 also activates the rat and mouse GPR139 receptor with similar potency (rat EC50 = 63 ± 24 nM, mouse EC50 = 28 ± 7 nM).

体内研究：

The small-molecule JNJ-63533054 is found to be devoid of any cross-reactivity as judged by an external selectivity panel of 50 known GPCRs, ion channels, and transporters, and it displays suitable pharmacokinetic properties for in vivo studies. JNJ-63533054 crosses the rat blood-brain barrier after oral administration and achieves exposure in the micromolar range. JNJ-63533054 administration decreases spontaneous locomotor activity in rats.

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