JNJ-63533054

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Chemical Structure| 1802326-66-4 同义名 : -
CAS号 : 1802326-66-4
货号 : A159562
分子式 : C17H17ClN2O2
纯度 : 99%+
分子量 : 316.78
MDL号 : MFCD29924732
存储条件：

Pure form Sealed in dry, room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
描述 GPR139 is an orphan G-protein–coupled receptor enriched in the Habenula and Septum. JNJ-63533054 is a potent, selective, small-molecule GPR139 agonist. It activated human GPR139 in the calcium mobilization and GTPgS binding assays with EC50 values of 16±6 and 17±4nM, respectively. JNJ-63533054 also activated rat and mouse GPR139 receptors with EC50 values of 63±24 and 28±7nM, respectively. The inhibition equilibrium constants (Ki) of JNJ-63533054 for binding to the membrane of cells expressing human, rat or mouse GPR139 are 23±3, 75±25, 54±12nM, respectively. L-Trp and L-Phe competed for [3H]JNJ-63533054 binding sites in T-REx CHO cells expressing human GPR139 with Ki values of 738±64 and 872±7μM, respectively. In Sprague-Dawley rats, JNJ-63533054 at dosages of 3, 10, and 30mg/kg induced a dose-dependent reduction in locomotor activity in the first hour after the treatment when compared with the vehicle-treated group[3].
作用机制 JNJ-63533054 is a potent agonist of GPR139, an orphan G protein-coupled receptor expressed in the central nervous system[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.16mL

0.63mL

0.32mL

15.78mL

3.16mL

1.58mL

31.57mL

6.31mL

3.16mL
参考文献

[1]Liu C, Bonaventure P, 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.

[2]Dvorak CA, Coate H, 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.

[3]Liu C, Bonaventure P, Lee G, 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;88(5):911-925.