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GNE-9605
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GNE-9605图片
CAS NO:1536200-31-3
规格:98%
分子量:449.83
包装与价格:
包装价格(元)
5mg电议
25mg电议

产品介绍
LRRK2 inhibitor, brain-penetrant, potent and selective
CAS:1536200-31-3
分子式:C17H20ClF4N7O
分子量:449.83
纯度:98%
存储:Store at -20°C

Background:

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:
[1].  Estrada AA, Chan BK, Baker-Glenn C, et al. Discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. J Med Chem, 2014, 57(3): 921-936.