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JNJ-5207787 is a penetrates the blood-brain barrier neuropeptide Y Y2 receptor (Y2) antagonist. It is >100-fold selective versus human Y1, Y4, and Y5 receptors. JNJ-5207787 suppresses the binding of peptide YY with pIC50s of 7.0 and 7.1 for the human Y2 receptor and rat Y2 receptor, respectively.
JNJ-5207787 is a penetrates the blood-brain barrier neuropeptide Y Y2 receptor (Y2) antagonist. It is >100-fold selective versus human Y1, Y4, and Y5 receptors. JNJ-5207787 suppresses the binding of peptide YY with pIC50s of 7.0 and 7.1 for the human Y2 receptor and rat Y2 receptor, respectively.
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 770 | 35日内发货 | |
10 mg | ¥ 5,180 | 35日内发货 |
产品描述 | JNJ-5207787 is a penetrates the blood-brain barrier neuropeptide Y Y2 receptor (Y2) antagonist. It is >100-fold selective versus human Y1, Y4, and Y5 receptors. JNJ-5207787 suppresses the binding of peptide YY with pIC50s of 7.0 and 7.1 for the human Y2 receptor and rat Y2 receptor, respectively. |
靶点活性 | Y2 receptor (rat):7.1 (pic50), Y2 receptor (human):7.0 (pic50) |
体外活性 | JNJ-5207787 (10 μM; 15 min) suppresses [125I]PYY labeling in the lateral septum, cerebellum, ventral tegmental area, substantia nigra, hippocampus, septum, amygdala, and hypothalamus. JNJ-5207787 (0.01, 0.1, 1, 10 μM) has antagonistic properties and suppresses the PYY-stimulated [35S]GTPγS binding to basal level with a p IC50 corr of 7.20 [1]. |
体内活性 | JNJ-5207787 (i.p.; 30 mg/kg) penetrates the brain (Cmax=1351 ng/ml at 30 min) and occupies Y2 receptor binding sites[1]. |
分子量 | 510.67 |
分子式 | C32H38N4O2 |
CAS No. | 683746-68-1 |
密度 | 1.22 g/cm3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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