GNE-0877CAS号： 1374828-69-9分子式： C14H16F3N7分子量： 339.32描述纯度储存/保存方法可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)参考文献
| 产品描述 | |
| 描述 |
GNE-0877 is a highly potent and selective leucine-rich repeat kinase 2 (LRRK2) inhibitor with Ki of 0.7 nM.
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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 | |
| 可溶性/溶解性 |
DMSO:67 mg/mL (197.45 mM)
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| 生物活性 | |
| 靶点 |
LRRK2
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| In vitro(体外研究) |
GNE-0877 significantly inhibits LRRK2 cellular activity with IC50 of 3 nM, and shows low turnover in human liver microsomes and hepatocytes. Besides, GNE-0877 is also a reversible CYP1A2 inhibitor with IC50 of 0.7 μM.
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| In vivo(体内研究) |
In vivo, GNE-0877 shows good oral bioavailability and brain penetration. GNE-0877 inhibits in vivo LRRK2 Ser1292 autophosphorylation in BAC transgenic mice expressing human LRRK2 protein with the G2019S Parkinson’s disease mutation.
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| 参考文献 | |
| 参考文献 |
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分子结构图
