Information GNE-9605 GNE-9605 is a highly potent and selective leucine-rich repeat kinase 2 (LRRK2) inhibitor with K i and IC50 of 2 nM and 19 nM, respectively. Targets LRRK2 ; LRRK2 2 nM(Ki); 19 nM In vitro GNE-9605 is highly potent against LRRK2 in both biochemical (Ki = 2.0 nM) and cellular (IC50 = 19 nM) assays. In vitro human MDR1 permeability data, GNE-9605 exhibits excellent brain penetration in higher species. In vivo In vivo rat PK studies with GNE-9605 (1 mg/kg, p.o.) demonstrates a total plasma clearance of 26 mL/min/kg with excellent oral bioavailability (90%). In BAC transgenic mice expressing human LRRK2 protein with the G2019S Parkinson’s disease mutation, GNE-9605 (10 and 50 mg/kg, i.p.) inhibits in vivo LRRK2 Ser1292 autophosphorylation.
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GNE-9605
Dangerous GoodsCAS number：1536200-31-3 molecular formula：C17H20ClF4N7O
overview
compound introduction
Specs
| Chinese alias | - | ||
| English alias | GNE9605 | N2-(5-chloro-1-((3S,4S)-3-fluoro-1-(oxetan-3-yl)piperidin-4-yl)-1H-pyrazol-4-yl)-N4-methyl-5-(trifluoromethyl)pyrimidine-2,4-diamine | ||
| CAS number | 1536200-31-3 | molecular formula | C17H20ClF4N7O |
| molecular weight | 449.83 g/mol | Exact mass | - |
| PSA | 80.100 Ų | logp | 2.715 |
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physicochemical properties
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Safety information
pictogram：
GHS07
Signal word：
Warning
Hazard Statement：
H302: 吞食有害
Statement of Preventive Measures：
P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。
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