ADL-5859 - Opioid Receptor Agonist - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEADL-5859Cat. No.: HY-13044CAS No.: 850173-95-4分式: CHClNO分量: 428.95作靶点: Opioid Receptor作通路: GPCR/G Protein; Neuronal Signaling储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (233.1

2、3 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.3313 mL 11.6564 mL 23.3127 mL5 mM 0.4663 mL 2.3313 mL 4.6625 mL10 mM 0.2331 mL 1.1656 mL 2.3313 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠

3、性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.75 mg/mL (6.41 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.75 mg/mL (6.41 mM); Clear solution1/2 Master of Small Molecules 您

4、边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 ADL5859-阿受体选择性激动剂，Ki为0.8 nM，对hERG有弱抑制性。户使本产品发表的科研献 Eur J Pharmacol. 2016 Jun 15;781:53-9.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Nozaki C, et al. -Opioid Mechanisms for ADL5747 and ADL5859 Effects in Mice: Analgesia, Locomotion,

5、and Receptor Internalization.JPharmacol Exp Ther. 2012 Sep;342(3):799-807.2. Le Bourdonnec B, et al. Spirocyclic delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-3-hydroxy-4-(spirochromene-2,4-piperidine-4-yl) benzamide (ADL5747).J Med Chem. 2009 Sep 24;52(18):5685-

6、702.3. Le Bourdonnec B, Windh RT, Ajello CW, Leister LK, Gu M, Chu GH, Tuthill PA, Barker WM, Koblish M, Wiant DD, Graczyk TM,Belanger S, Cassel JA, Feschenko MS, Brogdon BL, Smith SA, Christ DD, Derelanko MJ, Kutz S, Little PJ, DeHaven RN, DeHaven-Hudkins DL,4. Le Bourdonnec B et al. Potent, orally

7、 bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspirochromene-2,4-piperidine-4-yl)benzamide (ADL5859) J Med Chem. 2008 Oct 9;51(19):5893-6.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use on