Chemical Structure : LY2817412
CAS No.:
1307245-95-9
LY2817412
(LY 2817412)
Catalog No.: PC-21793Not For Human Use, Lab Use Only.
LY2817412 is a potent, selective andorally active nociceptin/orphanin FQ (NOP) receptor antagonist with Ki of 0.176 nM, Kb of 0.273 nM in functional assay of receptor-mediated G-protein activation using [35S]-GTPγS binding.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
LY2817412 is a potent, selective andorally active nociceptin/orphanin FQ (NOP) receptor antagonist with Ki of 0.176 nM, Kb of 0.273 nM in functional assay of receptor-mediated G-protein activation using [35S]-GTPγS binding.
LY2817412 shows high selectivity versus mu, kappa, and delta opioid receptors was also excellent (Ki > 375 nM).
LY2817412 reduces voluntary alcohol drinking in male and female msP rats.
Physicochemical Properties
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M.Wt
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468.92
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Formula
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C21H20ClF3N4OS
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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2'-chloro-4',4'-difluoro-1-((1-(3-fluoropyridin-2-yl)-3-methyl-1H-pyrazol-4-yl)methyl)-4',5'-dihydrospiro[piperidine-4,7'-thieno[2,3-c]pyran]
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References
1. Miguel A Toledo, et al. J Med Chem. 2014 Apr 24;57(8):3418-29.
2. Kallupi M, et al. Neuropsychopharmacology. 2017 Feb;42(3):695-706.
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