Immunoway/GNE-7915/10mg 50mg 100mg/MC0495
市场价：
¥4080.00
美元价：
2040.00
联系Q Q：
3392242852
电话号码：
4000-520-616
电子邮箱：
info@ebiomall.com
商品介绍
GNE-7915
- Catalog No.：MC0495
- Data Sheet
- MSDS
- Support
- Description
- References ( 0 )
- Protocol
- CasNo：
- 1351761-44-8
- MolecularFormula：
- C19H21F4N5O3
- Purity：
- >98%
- Target：
- LRRK2
- IC50：
- IC50: 9 nM[1] (LRRK2)
- In Vitro：
- 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[2].
- In Vivo：
- Fields：
- 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).
- Specificity：
- Target:LRRK2. Fields: 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
- Source：
- Rabbit
- Dilution：
- IC50: 9 nM[1] (LRRK2)
- Concentration：
- >98%
- Storage Stability：
- 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO
- Other Name：
- GNE7915; GNE 7915
- MolecularWeight(Da)：
- 443.4
- References：
- [1]. Kavanagh ME, et al. The development of CNS-active LRRK2 inhibitors using property-directed optimisation. Bioorg Med Chem Lett. 2013 Jul 1;23(13):3690-6.[2]. Estrada AA, et al. Discovery of highl
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