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LY2795050

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LY2795050
结构式
1346133-08-1
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中国地区超过5000个高品质化合物库存
应用领域
LY2795050是高活性κ-阿片受体（KOR）拮抗剂，IC50为0.72 nM。
化学性质生物活性化合物的使用COA & MSDS相关产品产品说明书
Cas No.: 1346133-08-1
名称: (S)-3-chloro-4-(4-((2-(pyridin-3-yl)pyrrolidin-1-yl)methyl)phenoxy)benzamide
别名: LY2795050,LY 2795050,LY-2795050,1346133-08-1
SMILES: O=C(N)C1=CC=C(OC2=CC=C(CN3[C@H](C4=CC=CN=C4)CCC3)C=C2)C(Cl)=C1
分子式: C23H22ClN3O2
分子量: 407.14
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: LY2795050 is a novel selective κ-opioid Receptor (KOR) antagonist (IC50=0.72 nM) and has the potential as a PET tracer to image KOR in vivo. IC50 Value: 0.72 nM (κ-opioid Receptor); 25.8 nM (κ-opioid) [1] Target: κ-opioid Receptor 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 . 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.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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