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产品详情
产品名称 英文名称:LY2795050 同义词 LY2795050、1346133-08-1、LY-2795050、71PAL357HO、CHEMBL1921842、Benzamide, 3-chloro-4-(4-(((2S)-2-(3-pyridinyl)-1-pyrrolidinyl)methyl)phenoxy)-benzamide, 3-chloro-4-(4-(((2S)-2-(3-pyridinyl)-1-pyrrolidinyl)methyl)phenoxy)-、3-Chloro-4-[4-[[(2S)-2-pyridin-3-ylpy 产品性质 CAS编号:1346133-08-1 分子式:C23H22ClN3O2 分子量:407.89 PubChem编号:56851583 英文别名:LY2795050|1346133-08-1|LY-2795050|71PAL357HO|CHEMBL1921842|Benzamide, 3-chloro-4-(4-(((2S)-2-(3-pyridinyl)-1-pyrrolidinyl)methyl)phenoxy)-benzamide, 3-chloro-4-(4-(((2S)-2-(3-pyridinyl)-1-pyrrolidinyl)methyl)phenoxy)-|3-Chloro-4-[4-[[(2S)-2-pyridin-3-ylpy 英文名称:LY2795050 生化机理:DescriptionIC50 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 MORKOR was 7.6 [2].Clinical trial N/A 储存温度:-20°C储存 运输条件:超低温冰袋运输 IUPAC Name:3-chloro-4-[4-[[(2S)-2-pyridin-3-ylpyrrolidin-1-yl]methyl]phenoxy]benzamide INCHI:InChI=1S/C23H22ClN3O2/c24-20-13-17(23(25)28)7-10-22(20)29-19-8-5-16(6-9-19)15-27-12-2-4-21(27)18-3-1-11-26-14-18/h1,3,5-11,13-14,21H,2,4,12,15H2,(H2,25,28)/t21-/m0/s1 InChi Key:LOOCZNLSXJHWTG-NRFANRHFSA-N Canonical SMILES:C1CC(N(C1)CC2=CC=C(C=C2)OC3=C(C=C(C=C3)C(=O)N)Cl)C4=CN=CC=C4 Isomeric SMILES:C1C[C@H](N(C1)CC2=CC=C(C=C2)OC3=C(C=C(C=C3)C(=O)N)Cl)C4=CN=CC=C4 PubChem CID:56851583 溶解性:25°C DMSO 产品包装
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