S80996 |
ADL5859 HCl |
源叶(MedMol) | 98% |
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- 产品描述: ADL-5859 (compound 20) is a selective and orally active δ opioid receptor (DOR) agonist with an Ki and an EC50 value of 0.84 and 20 nM, respectively. ADL-5859 also shows inhibitory activity to hERG channel with an IC50 value of 78 μM. ADL-5859 can be used for the research of pain
- 靶点: IC50: 78 μM (hERG channel), 43 μM (CYP2D6);OpioidReceptor
- 体内研究:
ADL-5859 (0.3-10 mg/kg; p.o. once) reverses hyperalgesia in inflamed paw of rats and shows robust antidepressant-like activity
- 参考文献:
1. Le Bourdonnec B, et al. Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide (ADL5859). J Med Chem. 2008 Oct 9;51(19):5893-6. 2. Le Bourdonnec B, et al. Spirocyclic delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-3-hydroxy-4-(spiro[chromene-2,4'-piperidine]-4-yl) benzamide (ADL5747).J Med Chem. 2009 Sep 24;52(18):5685-702.
- 溶解性: Soluble in DMSO、H2O
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.331 ml 11.656 ml 23.312 ml 5 mM 0.466 ml 2.331 ml 4.662 ml 10 mM 0.233 ml 1.166 ml 2.331 ml 50 mM 0.047 ml 0.233 ml 0.466 ml
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