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首页-小分子抑制剂&激动剂-GPCR-Opioid Receptor-LY2817412
LY2817412

Chemical Structure : LY2817412

CAS No.: 1307245-95-9

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LY2817412 (LY 2817412)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 468.92
分子式 C21H20ClF3N4OS
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

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]

参考文献

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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