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ADL-5859

产品编号 T6175Cas号 850173-95-4
别名 ADL5859 Hydrochloride, ADL5859 HCl

ADL-5859 (ADL5859 Hydrochloride) 是δ-阿片受体选择性激动剂,Ki 为0.8 nM,对阿片受体 κ 和 μ 具有选择性。

ADL-5859

ADL-5859

纯度: 99.71%
产品编号 T6175 别名 ADL5859 Hydrochloride, ADL5859 HClCas号 850173-95-4

ADL-5859 (ADL5859 Hydrochloride) 是δ-阿片受体选择性激动剂,Ki 为0.8 nM,对阿片受体 κ 和 μ 具有选择性。

规格价格库存数量
1 mg¥ 378现货
2 mg¥ 556现货
5 mg¥ 972现货
10 mg¥ 1,630现货
25 mg¥ 3,220现货
50 mg¥ 4,690现货
100 mg¥ 6,720现货
500 mg¥ 13,500现货
1 mL x 10 mM (in DMSO)¥ 1,060现货
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纯度:99.71%
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产品介绍

生物活性
产品描述
ADL-5859 (ADL5859 Hydrochloride) is a selective δ-opioid receptor agonist ( Ki: 0.8 nM), selectivity against opioid receptor κ, μ, and little inhibition for the hERG channel.
靶点活性
κ opioid receptor:37 nM(Ki), δ opioid receptor:0.8 nM(Ki), μ opioid receptor:32 nM(Ki)
体外活性
ADL5859是一种具有1000倍选择性的δ-阿片受体激动剂,在δ-阿片受体上的Ki值分别为32 nM和37 nM。ADL5859对hERG通道的抑制活性较弱,其IC50为78 μM。ADL5859针对δ阿片受体的EC50为20 nM。[1]
体内活性
在3 mg/kg口服剂量的筛选下, ADL5859能够完全逆转炎症爪部的高敏反应。ADL5859在FCA机械高敏反应测定中的口服ED50为1.4 mg/kg。通过预处理δ阿片受体拮抗剂纳曲酮(0.3 mg/kg皮下注射),ADL5859(3 mg/kg, 口服)产生的抗高敏效应被逆转,从而证明了δ受体介导的效应。在大鼠强迫游泳试验中,ADL5859(3 mg/kg口服)产生显著的抗抑郁样活动,表现为显著减少静止时间并显著增加游泳时间。ADL5859(3 mg/kg口服)在大鼠和狗中的生物利用度分别为33%和66%。ADL5859通过招募外周Nav1.8表达神经元所表达的δ-阿片受体,高效减轻炎症性及神经病理性疼痛。
细胞实验
Membrane preparations from Chinese hamster ovary (CHO) cells stably expressing human κ, μ, or δ opioid receptors are prepared. The assay buffer used is composed of 50 mMtris(hydroxymethyl) aminomethaneHCl, pH 7.8, 1.0 mM ethylene glycol bis(β-aminoethyl ether)-N,N,N',N'-tetraacetic acid (EGTA free acid), 5.0 mM MgCl2 10 mg/L leupeptin, 10 mg/L pepstatin A, 200 mg/L bacitracin, and 0.5 mg/L aprotinin. After dilution in assay buffer and homogenization in a Polytron homogenizer for 30 seconds, membrane proteins (10-80 μg) in 250 μL of assay buffer are added to mixtures containing ADL5859 and [3H]diprenorphine (0.5-1.0 nM, 25000-50000 dpm) in 250 μL of assay buffer in 96-well deep-well polystyrene titer plates and incubated at room temperature for 60 minutes. Reactions are terminated by vacuum filtration with a Brandel MPXR-96T harvester through GF/B filters that have been pretreated with a solution of 0.5% polyethylenimine and 0.1% bovine serum albumin for at least 1 hour. The filters arewashed four times with 1.0 mL each of ice-cold 50 mM Tris-HCl, pH 7.8, and 30 μL of Microscint-20 is added to each filter. Radioactivity on the filters is determined by scintillation spectrometry in a Packard TopCount. [3H]Diprenorphine with a specific activity of 50 Ci/mmolisused. The Kd values for [3H]diprenorphine binding are 0.33 nM for the κ and μ receptors and 0.26 nM for the δ receptor. Receptor expression levels, determined as Bmax values from Scatchard analyses, are 4400, 4700, and 2100 fmol/mg of protein for the κ, μ, and δ receptors, respectively. Preliminary experiments are performed to show that no specific binding is lost during the wash of the filters, that binding achieved equilibrium within the incubation time and remained at equilibrium for at least an additional 60 minutes, and that binding is linear with regard to protein concentration. Nonspecific binding, determined in the presence of 10 μM unlabeled naloxone, is less than 10% of total binding.Protein is quantified by the method of Bradford. The data from competition experiments are fit by nonlinear regression analysis with the program Prism using the four-parameter equation for one-site competition, and Ki values are subsequently calculated from EC50 values by the Cheng-Prusoff equation.(Only for Reference)
别名ADL5859 Hydrochloride, ADL5859 HCl
化学信息
分子量428.95
分子式C24H28N2O3·HCl
CAS No.850173-95-4
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
H2O: 5 mg/mL (11.65 mM)
DMSO: 35 mg/mL (81.59 mM), Sonication is recommended.
Ethanol: 1 mg/mL (2.33 mM)
溶液配制表
Ethanol/H2O/DMSO
1mg5mg10mg50mg
1 mM2.3313 mL11.6564 mL23.3127 mL116.5637 mL
H2O/DMSO
1mg5mg10mg50mg
5 mM0.4663 mL2.3313 mL4.6625 mL23.3127 mL
10 mM0.2331 mL1.1656 mL2.3313 mL11.6564 mL
DMSO
1mg5mg10mg50mg
20 mM0.1166 mL0.5828 mL1.1656 mL5.8282 mL
50 mM0.0466 mL0.2331 mL0.4663 mL2.3313 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
%Tween 80
%ddH2O

剂量转换

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关键词

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