2307277-93-4

2307277-93-4 structure
2307277-93-4 structure
  • Name: LRRK2-IN-7
  • Chemical Name: LRRK2-IN-7
  • CAS Number: 2307277-93-4
  • Molecular Formula: C24H26N6O
  • Molecular Weight: 414.50
  • Catalog: Signaling Pathways Autophagy LRRK2
  • Create Date: 2023-01-31 16:06:01
  • Modify Date: 2024-04-10 19:11:09
  • 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].

Name LRRK2-IN-7
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

[1]. David A Candito, et al. Discovery and Optimization of Potent, Selective, and Brain-Penetrant 1-Heteroaryl-1 H-Indazole LRRK2 Kinase Inhibitors for the Treatment of Parkinson's Disease. J Med Chem. 2022 Dec 22;65(24):16801-16817.  

Molecular Formula C24H26N6O
Molecular Weight 414.50