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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-GABA Receptor-GR3027
GR3027

Chemical Structure : GR3027

CAS No.: 2089238-18-4

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GR3027 (GR-3027, Golexanolone)

货号: PC-35454Not For Human Use, Lab Use Only.

GR3027 (Golexanolone) is a GABA-A receptor modulating steroid antagonist that selectively antagonizes the enhanced activation of GABAA receptors by neurosteroids such as allopregnanolone and THDOC.

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

    生物&药学活性

    GR3027 (Golexanolone) is a GABA-A receptor modulating steroid antagonist that selectively antagonizes the enhanced activation of GABAA receptors by neurosteroids such as allopregnanolone and THDOC.
    GR3027 inhibits α1β2γ2L receptor 29 ± 5% of THDOC enhancement of the GABA response, does not antagonize the effect of GABA at the GABAA receptor.
    GR3027 during the specific conditions used for the different receptors, IC50=250 nM for the α1β2γ2L GABAA receptor and 350 nM for the α5β3γ2L GABAA receptor.
    GR3027 restores spatial learning and motor coordination in rats with chronic hyperammonemia and hepatic encephalopathy.

    物理化学性质&存储条件

    分子量 329.48
    分子式 C21H31NO2
    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

    (17E)-3α-ethynyl-17-(hydroxyimino)-5α-androstan-3β-ol

    参考文献

    1. Johansson M, et al. Am J Physiol Gastrointest Liver Physiol. 2015 Sep 1;309(5):G400-9.

    2. Johansson M, et al. J Steroid Biochem Mol Biol. 2016 Jun;160:98-105.

    3. Johansson M, et al. Psychopharmacology (Berl). 2018 May;235(5):1533-1543.

    4. Patent WO 2008/063128.

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