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
货号 品牌 包装 目录价 您的价格 库存 数量 购买
L125659-100mg 阿拉丁 100mg ¥12472.90
L125659-10mg 阿拉丁 10mg ¥2602.90
L125659-25mg 阿拉丁 25mg ¥5204.90
L125659-50mg 阿拉丁 50mg ¥8017.90
L125659-5mg 阿拉丁 5mg ¥1592.90
产品名称 LY2795050
中文名称 LY2795050,κ-阿片受体(KOR)拮抗剂
CAS号 1346133-08-1
储存条件 -20°C储存
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
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