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JNJ-5207787
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-5207787图片
CAS NO:683746-68-1
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
JNJ-5207787 是一种非肽类,选择性且可穿透血脑屏障的神经肽 Y Y2受体 (Y2)拮抗剂。JNJ-5207787 抑制 YY 肽 (PYY) 和人 Y2受体,大鼠 Y2受体结合,pIC50分别为 7.0 和 7.1。JNJ-5207787 相对于人 Y1,Y4和 Y5受体具有 >100 倍的选择性。
生物活性

JNJ-5207787 is a nonpeptidic, selective and penetrate the blood-brain barrierneuropeptide Y Y2receptor (Y2)antagonist. JNJ-5207787 inhibits the binding of peptide YY (PYY) withpIC50s of 7.0 and 7.1 for human Y2receptor and rat Y2receptor, respectively. JNJ-5207787 is >100-fold selective versus human Y1, Y4, and Y5receptors[1].

IC50& Target[1]

human Y2receptor

7.0 (pIC50)

rat Y2receptor

7.1 (pIC50)

体外研究
(In Vitro)

JNJ-5207787 (0.01, 0.1, 1, 10 μM) has antagonistic properties and inhibits the PYY-stimulated [35S]GTPγS binding to basal level with a p IC50corr of 7.20[1].
JNJ-5207787 (10 μM; 15 min) inhibits [125I]PYY labeling in lateral septum, cerebellum, ventral tegmental area, substantia nigra, hippocampus, septum, amygdala, and hypothalamus[1].

体内研究
(In Vivo)

JNJ-5207787 (i.p.; 30 mg/kg) penetrates into the brain (Cmax=1351 ng/ml at 30 min) and occupies Y2receptor binding sites[1].

Animal Model:Sixteen female Sprague-Dawley Rats (approximately 300 g of body weight)[1]
Dosage:30 mg/kg
Administration:IP
Result:Penetrated into the brain (Cmax=1351 ng/ml at 30 min) and occupied Y2receptor binding sites.
分子量

510.67

性状

Solid

Formula

C32H38N4O2

CAS 号

683746-68-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
In solvent-80°C6 months
-20°C1 month