溶解性 | 25°C: DMSO |
存贮条件 | 储存温度-20°C |
生化机理 | Description:IC50 Value: 0.72 nM (κ-opioid Receptor); 25.8 nM (κ-opioid) [1]LY2795050 is a novel selective KOR antagonist and has the potential as a PET tracer to image KOR in vivo.in vitro: LY2795050 displays full antagonist activity and high binding affinity and selectivity for KOR with a ki value of 0.72 nM [1].in vivo: In the brain, (11)C-LY2795050 displayed fast uptake kinetics (regional activity peak times of <20 min) and an uptake pattern consistent with the distribution of KOR in primates [1]. The LY2795050 ED50 at MOR was 119 μg/kg based on a 1-site model for 11C-carfentanil. The 1-site binding model was also deemed sufficient to describe the specific binding of 11C-LY2795050 at KOR. The ED50 at KOR estimated from the 1-site model was 15.6 μg/kg. Thus, the ED50 ratio for MOR:KOR was 7.6 [2].Clinical trial: N/A |
LY2795050,κ-阿片受体(KOR)拮抗剂
LY2795050 (订货以英文为准)
编号:L125659
CAS号:1346133-08-1
分子式:C23H22CLN3O2
分子量:407.89
产品名称 | LY2795050 |
中文名称 | LY2795050,κ-阿片受体(KOR)拮抗剂 |
CAS号 | 1346133-08-1 |
分子式(M.F.) | C23H22CLN3O2 |
分子量(M.W.) | 407.89 |
储存条件 | -20°C储存 |
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