| CAS NO: | 1536200-31-3 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 5mg | 电议 |
| 25mg | 电议 |
| Cas No. | 1536200-31-3 |
| 化学名 | 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 |
| Canonical SMILES | CNC1=NC(NC2=C(Cl)N([C@@H]3[C@@H](F)CN(C4COC4)CC3)N=C2)=NC=C1C(F)(F)F |
| 分子式 | C17H20ClF4N7O |
| 分子量 | 449.83 |
| 溶解度 | ≥ 22.5mg/mL in DMSO |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | GNE-9605 is a potent and selective inhibitor of LRRK2 with IC50 value of 19 nM [1]. Leucine-rich repeat kinase 2 (LRRK2) is a member of the leucine-rich repeat kinase family. Variants of LRRK2 gene are the most common cause of Parkinson's disease and Crohn's disease. GNE-9605 is a brain-penetrant, potent and selective LRRK2 inhibitor. GNE-9605 was highly potent against LRRK2 with Ki and IC50 values of 2.0 and 18.7 nM, respectively. In human hepatocytes and liver microsomes, GNE-9605 exhibited excellent human metabolic stability [1]. In rat pharmacokinetic (PK) studies, GNE-9605 exhibited excellent oral bioavailability of 90% and total plasma clearance of 26 mL/min/kg. In bacterial artificial chromosome (BAC) transgenic mice expressing human G2019S LRRK2 protein with the Parkinson’s disease mutation, GNE-9605 (10 or 50 mg/kg) inhibited LRRK2 Ser1292 autophosphorylation with IC50 value of 20 nM in a concentration dependent way. In cynomolgus monkey PK studies, GNE-9605 exhibited excellent brain penetration [1]. Reference: |
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