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首页-小分子抑制剂&激动剂-GPCR-Opioid Receptor-W-212393
W-212393

Chemical Structure : W-212393

CAS No.: 610323-32-5

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W-212393 (W212393;MT-7716 free base)

货号: PC-61541Not For Human Use, Lab Use Only.

W-212393 (MT-7716 free base) is a highly potent, brain penetrant ORL1 receptor (NOP receptor) agonist with Ki of 0.76 and 0.50  nM for rat and human ORL1 receptors, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    W-212393 (MT-7716 free base) is a highly potent, brain penetrant ORL1 receptor (NOP receptor) agonist with Ki of 0.76 and 0.50  nM for rat and human ORL1 receptors, respectively.
    W-212393 displays a relative selectivity over μ receptor and serotonin transporter.
    W-212393 significantly suppresses the activity of spontaneously firing rat suprachiasmatic nucleus neurons at 100 nM.
    W-212393 induces a significant phase advance at circadian time 6 (CT6) and CT9, but not at other CTs, represents an interesting agent for the study of circadian rhythms.
    MT-7716 dose-dependently decreases GABAergic transmission and effectively blocks the ethanol-induced increase in GABA release at these synapses.

    物理化学性质&存储条件

    分子量 440.547
    分子式 C27H28N4O2
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20 °C 12 个月; 4°C 6 个月
    配置液
    -80 °C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO
    Chemical Name/SMILES

    2-{3-[1-((1R)-acenaphthen-1-yl)piperidin-4-yl]-2,3-dihydro-2-oxo-benzimidazol-1-yl}-N-methylacetamide

    参考文献

    1. Teshima K, et al. Br J Pharmacol. 2005 Sep;146(1):33-40.

    2. Miyakawa K, et al. Neuropharmacology. 2007 Mar;52(3):1055-64.

    3. Kallupi M, et al. Front Integr Neurosci. 2014 Feb 18;8:18.

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