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首页-小分子抑制剂&激动剂-GPCR-Orexin Receptor-GSK-1059865
GSK-1059865

Chemical Structure : GSK-1059865

CAS No.: 1191044-58-2

GSK-1059865 (GSK 1059865, GSK1059865)

货号: PC-60752Not For Human Use, Lab Use Only.

GSK-1059865 is a highly potent, selective orexin-1 receptor (OX1R) antagonist with IC50 of 5.0 and 6.4 nM for hOX1R and rOX1R, respectively.

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10 mg ¥2580 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GSK-1059865 is a highly potent, selective orexin-1 receptor (OX1R) antagonist with IC50 of 5.0 and 6.4 nM for hOX1R and rOX1R, respectively.
GSK-1059865 displays >80-fold selectivity over OX2R.
GSK-1059865 robustly inhibits the response in fronto-hippocampal regions in rats.
GSK-1059865 significantly decreases ethanol drinking in a dose-dependent manner in CIE-exposed mice.

物理化学性质&存储条件

分子量 436.325
分子式 C20H23BrFN3O2
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

5-bromo-N-({1-[(3-fluoro-2-methoxyphenyl)carbonyl]-5-methylpiperidin-2-yl}methyl)pyridin-2-amine

参考文献

1. Gozzi A, et al. PLoS One. 2011 Jan 28;6(1):e16406.

2. Gozzi A, et al. Neuropsychopharmacology. 2013 Oct;38(11):2120-30.

3. Aluisio L, et al. Front Neurosci. 2014 May 20;8:107.

4. Bonaventure P, et al. J Pharmacol Exp Ther. 2015 Mar;352(3):590-601.

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