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首页-小分子抑制剂&激动剂-GPCR-Neuropeptide Y Receptor-JNJ-31020028
JNJ-31020028

Chemical Structure : JNJ-31020028

CAS No.: 1094873-14-9

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JNJ-31020028 (JNJ31020028)

货号: PC-28418Not For Human Use, Lab Use Only.

JNJ-31020028 is a potent, selective, brain penetran antagonist of neuropeptide Y Y2 receptor (Y2R) with binding pIC50 of 8.07 and 8.22 for human and rat Y(2) receptors, >100-fold selective versus human Y(1), Y(4), and Y(5) receptors.

规格 价格 库存 数量
10 mg ￥580 In stock
25 mg ￥980 In stock
50 mg ￥1580 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

JNJ-31020028 is a potent, selective, brain penetran antagonist of neuropeptide Y Y2 receptor (Y2R) with binding pIC50 of 8.07 and 8.22 for human and rat Y(2) receptors, >100-fold selective versus human Y(1), Y(4), and Y(5) receptors.
JNJ-31020028 is an antagonist (pK(B) = 8.04 +/- 0.13) in functional assays.
JNJ-31020028 occupies Y(2) receptor binding sites (approximately 90% at 10 mg/kg) after subcutaneous administration in rats.
JNJ-31020028 increases norepinephrine release in the hypothalamus, consistent with the colocalization of norepinephrine and neuropeptide Y.
JNJ-31020028 reverses nicotine-induced social anxiety-like behavior.

物理化学性质&存储条件

分子量 565.69
分子式 C34H36FN5O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

N-(4-(4-(2-(Diethylamino)-2-oxo-1-phenylethyl)piperazin-1-yl)-3-fluorophenyl)-2-(pyridin-3-yl)benzamide

参考文献

1. Shoblock JR, et al. Psychopharmacology (Berl). 2010 Feb;208(2):265-77.

2. Swanson DM, et al. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5552-6.

3. Cippitelli A, et al. Alcohol. 2011 Sep;45(6):567-76.

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