Name | LRRK2-IN-7 |
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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]. |
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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 |
Molecular Formula | C24H26N6O |
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Molecular Weight | 414.50 |