LRRK2-IN-7 is a potent, selective, and CNS-penetrant LRRK2 kinase inhibitor with an IC 50 of 0.9 nM. LRRK2-IN-7 shows >1000-fold selectivity over other kinases, ion channels, and CYP enzymes
In Vitro
LRRK2-IN-7 (compound 25) is both a mouse breast cancer resistance protein (BCRP) substrate (mouse/human BCRP) and a potent human BCRP inhibitor (BCRP IC 50 = 0.12 μM). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
In a 7 day rat dose limiting toxicity study, LRRK2-IN-7 (compound 25) is tolerated with no significant histopathology findings up to 100 mg/kg once a day (AUC tot = 330 μM·h) . In an acute (2 h) rat PK/PD study, LRRK2-IN-7 (compound 25) demonstrates a dose-dependent decrease in LRRK2 pS935 in rat brain striatum with an EC 50 = 0.18 nM . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
