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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
包装与价格:
包装价格(元)
5 mg电议
10 mg电议
50 mg电议
100 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
JNJ 63533054
产品介绍
JNJ63533054 是一种选择性的,具有口服活性的GPR139激动剂,对人GPR139的EC50为 16 nM。它可穿过血脑屏障,对 GPR139 的选择性高于其他 GPCR、离子通道和转运蛋白。

产品描述

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

体外活性

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.

体内活性

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).

Cas No.

1802326-66-4

分子式

C17H17ClN2O2

分子量

316.79

别名

JNJ 63533054

储存和溶解度

DMSO:31.7 mg/mL(100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years