(R,R)-LRRK2-IN-7 

(R,R)-LRRK2-IN-7 is the isomer of LRRK2-IN-7 (HY-152107). 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.

IC50: 0.9 nM (LRRK2 Kinase)^[1]

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 IC₅₀ = 0.12 μM)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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)^[1].
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 EC₅₀ = 0.18 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

414.50

C₂₄H₂₆N₆O

2307277-92-3

Solid

Light yellow to yellow

CC(C)(O)[C@@H]1CCN(C1)C2=NC=NC(N3C4=CC([C@]5(CC56CC6)C#N)=CC=C4C=N3)=C2

Room temperature in continental US; may vary elsewhere.

• [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.  [Content Brief]