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  • ADL5859 Hydrochloride

    • ADL5859 HCl
    货号: abs813298
    CAS号: 850173-95-4
    分子式: C24H28N2O3.HCl
    分子量: 428.95
    产品说明书
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    货号-规格 货期 价格 数量
    abs813298-5mg 1-2周 ¥1359.00
    - +
    abs813298-10mg 1-2周 ¥2450.00
    - +
    abs813298-25mg 1-2周 ¥4754.00
    - +
    abs813298-50mg 1-2周 ¥7883.00
    - +
    大包装询价
    产品描述
    描述

    ADL5859 HCl是一种δ-opioid receptor激动剂,Ki为0.8 nM,选择性作用于opioid receptor κ,μ,对hERG通道具有微弱的抑制活性。在32nM和37nM Ki 条件下ADL5859独立刺激δ-阿片类受体的特异选择性比µ-或者κ-阿片类受体高1000倍。在78uM IC50条件下,ADL5859表现出对hERG通道的弱的抑制效应。ADL5859对δ-阿片类受体的EC50值是20nM 。

    纯度
    98%
    储存/保存方法
    Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
    基本信息
    别名
    ADL5859 HCl
    可溶性/溶解性
    Ethanol :1 mg/mL (2.33 mM)

    DMSO :80 mg/mL (186.5 mM)

    Water :5 mg/mL (11.65 mM)
    生物活性
    靶点
    δ-opioid receptor,μ-opioid receptor,κ-opioid receptor
    In vitro(体外研究)
    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(体内研究)
    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.
    参考文献
    参考文献
    δ-Opioid mechanisms for ADL5747 and ADL5859 effects in mice: analgesia, locomotion, and receptor internalization.
    Nozaki C,et al. J Pharmacol Exp Ther. 2012 Sep;342(3):799-807. PMID:
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