5MG
中文名称 | 5MG |
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中文同义词 | |
英文名称 | GNE-7915 (tosylate) |
英文同义词 | GNE-7915 (tosylate);GNE-7915 tosylate (GNE7915 tosylate;CS-1278 |
CAS号 | 2070015-00-6 |
分子式 | C26H29F4N5O6S |
分子量 | 615.6 |
EINECS号 | |
相关类别 | |
Mol文件 | 2070015-00-6.mol |
结构式 |
5MG 性质
储存条件 | Store at -20°C |
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溶解度 | DMSO:≥50mg/mL(81.22mM);水:< 0.1 mg/mL(不溶) |
形态 | 固体 |
颜色 | 白色至米白色 |
IC50: 9 nM (LRRK2)
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-HT 2B with >70% inhibition at 10 μM. GNE-7915 and 19 are confirmed to be moderately potent 5-HT 2B antagonists in vitro functional assays.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | HY-18163A | GNE-7915 tosylate | 2070015-00-6 | 5 mg | 500元 |
2024/08/19 | HY-18163A | GNE-7915 tosylate | 2070015-00-6 | 10mM * 1mLin DMSO | 677元 |