产品信息
抗原名称
GPR139
商品描述
JNJ-63533054 is a potent and selective agonist of hGPR139 with an EC50 = 16 nM.
分子量
316.78
纯度
>98%
可溶性
DMSO : ≥ 50 mg/mL (157.84 mM)
外观
white to beige powder
In vitro(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 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.
In vivo(体内研究)
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. JNJ-63533054 also activates the rat and mouse GPR139 receptor with similar potency (rat EC50 = 63 ± 24 nM, mouse EC50 = 28 ± 7 nM).
背景
分子式
C17H17ClN2O2
CAS号
1802326-66-4
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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