GNE-7915 tosylate
- GNE7915 tosylate;GNE 7915 tosylate
货号: abs818930
货号-规格 | 货期 | 价格 | 数量 |
abs818930-10mg | 1-2周 | ¥1940.00 | - + |
abs818930-50mg | 1-2周 | ¥5579.00 | - + |

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 | ||
温馨提示:本产品仅作科研实验使用,不支持临床等研究 |
- 实验方法 实验条件
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