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CAS No.: 1351761-44-8

GNE-7915 Catalog No. CSN17181

Synonyms: GNE-7915

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

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生物活性

实验方案

技术信息

生物活性

描述The LRRK2 gene, which encodes a large, multidomain protein, is involved in Parkinson's disease pathophysiogenesis. GNE-7915 is a potent, selective and brain-penetrant inhibitor of LRRK2 with IC₅₀ and K_i of 9 and 1 nM, respectively. Cerep receptor profiling, including expanded brain panels, suggested that GNE-7915 inhibited 5-HT_2B with >70% inhibition at 10 μM. It was confirmed to be moderately potent 5-HT_2B antagonist in in vitro functional assays^[3]. When treated with 1 μM GNE‐7915 for 2 h, there was a significant increase of PPR (pair‐pulse ratio). Single‐pulse‐evoked DA (dopamine) release was also enhanced. Thirty‐minute perfusion also increased DA release and the PPR recorded from the same site^[4]. Moreover, pretreatment with GNE-7915 for 24 h was able to prevent LRRK2 G2019S-induced mtDNA damage. Most strikingly, exposure to GNE-7915 for 6 h was able to restore mtDNA damage to control levels^[5].
细胞研究
Cell Data
Cell Lines Concentration Assay Type Time Activity Description Data Sources
HEK293 cells - Function assay - Inhibition of autophosphorylation of LRRK2 in human HEK293 cells, IC50=0.009 μM 22985112
参考文献

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
HEK293 cells	-	Function assay	-	Inhibition of autophosphorylation of LRRK2 in human HEK293 cells, IC50=0.009 μM	22985112

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2553 mL
- 11.2766 mL
- 22.5532 mL
- 5 mM
- 0.4511 mL
- 2.2553 mL
- 4.5106 mL
- 10 mM
- 0.2255 mL
- 1.1277 mL
- 2.2553 mL

技术信息

CAS号

1351761-44-8

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H21F4N5O3

运输

蓝冰

分子量

443.40

别名

GNE-7915

溶解度

DMSO	86.0 mg/mL (194.0 mM) warming
Water	insoluble

动物实验配方

5% DMSO+30% PEG 300+5% Tween 80+water

3.1 mg/mL

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