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。

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

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.

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).

1802326-66-4

C17H17ClN2O2

316.79

JNJ 63533054

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