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JNJ-63533054
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
JNJ-63533054图片
CAS NO:1802326-66-4
规格:98%
分子量:316.78
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
JNJ-63533054 is a potent and selective agonist of hGPR139 with an EC50 = 16 nM.
CAS:1802326-66-4
分子式:C17H17ClN2O2
分子量:316.78
纯度:98%
存储:Store at -20°C

Background:

JNJ-63533054 is a potent and selective agonist of hGPR139 with an EC50 = 16 nM.IC50 value: 16 nM (EC50)Target: hGPR139in vitro: JNJ-63533054 is a selective small-molecule agonist. JNJ-63533054 specifically activates human GPR139 in the calcium mobilization (EC50 = 16 ± 6 nM) and GTPγS binding (EC50 = 17 ± 4 nM) assays. [2] JNJ-63533054 is found to be clean of any cross reactivity as judged by an external selectivity panel of 50 known GPCRs, ion channels, and transporters as well as our own internal whole cell lead generation biology selectivity panel.[1]in vivo: JNJ-63533054 is found to cross the blood-brain barrier and have good drug-like properties amenable for oral dosing in rat. JNJ-63533054 exhibits good stability in both human and rat microsomes and high solubility in aqueous media, and no DDI potential was found. [1] JNJ-63533054 also activates the rat and mouse GPR139 receptor with similar potency (rat EC50 = 63 ± 24 nM, mouse EC50 = 28 ± 7 nM). [2]


参考文献:
[1]. Dvorak CA, et al. Identification and SAR of Glycine Benzamides as Potent Agonists for the GPR139 Receptor. ACS Med Chem Lett. 2015 Jul 20;6(9):1015-8.
[2]. Liu C, et al. GPR139, an Orphan Receptor Highly Enriched in the Habenula and Septum, Is Activated by the Essential Amino Acids L-Tryptophan and L-Phenylalanine. Mol Pharmacol. 2015 Nov;88(5):911-25.