GNE-7915CAS号： 1351761-44-8分子式： C19H21F4N5O3分子量： 443.4描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
| 产品描述 | |
| 描述 |
GNE-7915 is a highly potent, selective, and brain-penetrable LRRK2 small molecule inhibitor with IC50 of 9 nM in cellular LRRK2 assay; > 100 fold selectivity against a panel of 187 kianses(Ki).
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| 纯度 |
>98%
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| 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.
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| 基本信息 | |
| 别名 |
GNE7915; GNE 7915
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| 外观 |
Powder
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| 可溶性/溶解性 |
DMSO 22 mg/mL warmed (49.61 mM)
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| 生物活性 | |
| 靶点 |
LRRK2 ,LRRK2
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| In vitro(体外研究) |
GNE-7915 is also a moderately potent 5-HT2B antagonist according to in vitro functional assays. GNE-7915 demonstrates excellent in vitro DMPK with minimal turnover in human hepatocytes.
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| In vivo(体内研究) |
In rats, GNE-7915 demonstrates excellent in vivo PK profiles with long half-lives, good oral exposure and high passive permeability. GNE-7915 (50 mg/kg i.p. or p.o.) results in concentration-dependent knockdown of pLRRK2 in the brain of BAC transgenic mice expressing human LRRK2 protein with the G2019S Parkinson’s disease mutation.
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分子结构图
