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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-GABA Receptor-HZ-166
HZ-166

Chemical Structure : HZ-166

CAS No.: 612527-56-7

HZ-166 (HZ166)

货号: PC-35484Not For Human Use, Lab Use Only.

HZ-166 (HZ166) is a GABAA receptor subtype-selective benzodiazepine site ligand with preferential activity at α2- and α3-GABA(A) receptors.

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

    生物&药学活性

    HZ-166 (HZ166) is a GABAA receptor subtype-selective benzodiazepine site ligand with preferential activity at α2- and α3-GABA(A) receptors.
    HZ-166 displays a statistically significant higher affinity for receptors not containing the α1 subunit with a rank order of α5 (Ki=140nM) > α2 (Ki=269 nM) > α1 (Ki=382 nM).
    The Ki value of HZ166 for the α3β3γ2 combination (185± 47 nM) was statistically significantly lower than the Ki value observed for α1β3γ2 but not different from those of α2β3γ2 and α5β3γ2.
    HZ-166 is antihyperalgesic in mouse models of inflammatory and neuropathic pain.

    物理化学性质&存储条件

    分子量 356.385
    分子式 C21H16N4O2
    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

    Ethyl 8-ethynyl-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,5-a][1,4]diazepine-3-carboxylate

    参考文献

    1. Fischer BD, et al. Neuropharmacology. 2010 Dec;59(7-8):612-8.

    2. Di Lio A, et al. Neuropharmacology. 2011 Mar;60(4):626-32.

    3. Witkin JM, et al. Neuropharmacology. 2018 Jul 15;137:332-343.

    4. Rivas FM, et al. J Med Chem. 2009 Apr 9;52(7):1795-8.

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