计算溶液所需的质量、体积或浓度。
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
ADL5859是δ-阿片受体选择性激动剂，Ki为0.8 nM，对hERG有弱抑制性。A selective receptor agonist for the δ-opioid receptor
Information
ADL5859 HCl is aδ-opioid receptoragonist withKiof 0.8 nM, selectivity against opioid receptor κ, μ, and weak inhibitory activity at the hERG channel. Phase 2.
In vitro
ADL5859 agonizes δ-opioid receptor with a 1000-fold selectivity than µ- or κ-opioid receptor with Ki of 32 nM and 37 nM, respectively.ADL5859 displays weak inhibitory activity at the hERG channel with an IC50 of 78 μM. The EC50 of ADL5859 against δ opioid receptor is 20 nM.
In vivo
At the screening dose of 3 mg/kg p.o., ADL5859 produces 100% reversal of hyperalgesia in the inflamed paw. The oral ED50 of ADL5859 in the FCA mechanical hyperalgesia assay is 1.4 mg/kg. The antihyperalgesia produced by ADL5859 (3 mg/kg, p.o.) is reversed by pretreatment with the δ opioid antagonist naltrindole (0.3 mg/kg s.c.), thus demonstrating a δ receptor mediated effect.In the rat forced swim assay, ADL5859 (3 mg/kg p.o.) produces robust antidepressant-like activity, as evidenced by a significant decrease in the time spent immobile and a significant increase in the time spent swimming. The bioavailability of ADL5859 (3 mg/kg p.o.) in rats and dogs is 33% and 66%, respectively.ADL5859 efficiently reduces inflammatory and neuropathic pain mainly by recruiting δ-opioid receptors expressed by peripheral Nav1.8-expressing neurons.
Cell Data
cell lines：
Concentrations：0 nM-10 nM
Incubation Time：60 minutes
Powder Purity:≥99%
规格
别名
ADL5859 盐酸
英文别名
Benzamide, N,N-diethyl-4-(5-hydroxyspiro[2H-1-benzopyran-2,4'-piperidin]-4-yl)-, hydrochloride (1:1)
规格或纯度
10mM in DMSO
英文名称
ADL5859 HCl
生化机理
ADL5859 HCl 是一种δ-阿片受体激动剂，Ki为 0.8 nM，对阿片受体κ、μ 有选择性，对 hERG 通道有微弱的抑制活性。第 2 阶段
储存条件
-80℃储存
运输条件
特低温运输
作用类型
激动剂
名称和识别符
分子类型
小分子
Isomeric SMILES
CCN(CC)C(=O)C1=CC=C(C=C1)C2=CC3(CCNCC3)OC4=CC=CC(=C42)O.Cl
分子量
428.96
Reaxy-Rn
12257215
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=12257215&ln=
技术文档
高级数据
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 30 mg/mL (72.9 mM); Water: Insoluble; Ethanol: Insoluble;
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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