Chemical Structure : GSK-1059865
CAS No.: 1191044-58-2
Catalog No.: 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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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.
M.Wt | 436.325 | |
Formula | C20H23BrFN3O2 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
5-bromo-N-({1-[(3-fluoro-2-methoxyphenyl)carbonyl]-5-methylpiperidin-2-yl}methyl)pyridin-2-amine |
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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