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  • GNE-7915 tosylate

    • GNE7915 tosylate;GNE 7915 tosylate
    货号: abs818930
    CAS号: 2070015-00-6
    分子式: C26H29F4N5O6S
    分子量: 615.6
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    货号-规格 货期 价格 数量
    abs818930-10mg 1-2周 ¥1940.00
    - +
    abs818930-50mg 1-2周 ¥5579.00
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    大包装询价
    产品描述
    描述

    GNE-7915 tosylate is a potent, selective and brain-penetrant inhibitor of LRRK2 with an IC50 of 9 nM. 

    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
    GNE7915 tosylate;GNE 7915 tosylate
    可溶性/溶解性
    DMSO : ≥ 50 mg/mL (81.22 mM)
    生物活性
    靶点
    LRRK2
    In vitro(体外研究)
    Maintaining the methoxy/fluoro arrangement at C-2′/C-5′ and varying aminoalkyl R1 substitution resultes in single-digit nanomolar LRRK2 cellular activities for GNE-7915 and compound 19. Expanded Invitrogen kinase profiling (187 kinases) at 0.1 μM for both GNE-7915 (100-fold over LRRK2 Ki) and 19 (250-fold over LRRK2 Ki) resultes in only TTK showing greater than 50% inhibition. Selectivity profiling using the DiscoverX KinomeScan55 competitive binding assay panel, which includes 392 unique kinases, is also performed for GNE-7915 at 0.1 μM. Binding of >50% probe displacement is detected for 10 kinases and of >65% for only LRRK2, TTK, and ALK, further supporting the excellent LRRK2 selectivity for GNE-7915. Cerep receptor profiling, including expanded brain panels, suggestes that GNE-7915 and 19 only inhibite 5-HT2B with >70% inhibition at 10 μM. GNE-7915 and 19 are confirmed to be moderately potent 5-HT2B antagonists in vitro functional assays.
    参考文献
    参考文献
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