LRRK2-IN-7
Names
[ CAS No. ]:
2307277-93-4
[ Name ]:
LRRK2-IN-7
Biological Activity
[Description]:
LRRK2-IN-7 is a potent, selective, and CNS-penetrant LRRK2 kinase inhibitor with an IC50 of 0.9 nM. LRRK2-IN-7 shows >1000-fold selectivity over other kinases, ion channels, and CYP enzymes[1].
[Related Catalog]:
[Target]
IC50: 0.9 nM (LRRK2 Kinase)[1]
[In Vitro]
LRRK2-IN-7 (compound 25) 既是小鼠乳腺癌抗性蛋白 (BCRP) 底物(小鼠/人 BCRP)也是一种有效的人 BCRP 抑制剂(BCRP IC50 = 0.12 μM)[1] .
[In Vivo]
在一项为期 7 天的大鼠剂量限制毒性研究中,LRRK2-IN-7 (compound 25) 的耐受性高达 100 mg/kg,每天一次(AUCtot = 330 μM·h)[1]。 在大鼠急性(2 小时)PK/PD 研究中,LRRK2-IN-7 (compound 25) 显示大鼠脑纹状体中 LRRK2 pS935 剂量依赖性降低,EC50 = 0.18 nM[1]。
[References]
Chemical & Physical Properties
[ Molecular Formula ]:
C24H26N6O
[ Molecular Weight ]:
414.50