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GSK-1059865

Chemical Structure : GSK-1059865

CAS No.: 1191044-58-2

GSK-1059865 (GSK 1059865;GSK1059865)

Catalog No.: PC-60752Not For Human Use, Lab Use Only.

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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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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

Physicochemical Properties

M.Wt 436.325
Formula C20H23BrFN3O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
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

References

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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