GNE-9605 is a highly potent and selective leucine-rich repeat kinase 2 (LRRK2) inhibitor with Ki and IC50 of 2 nM and 19 nM, respectively.
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of leucine rich repeat kinase 2
Product Description
Information
GNE-9605 GNE-9605 is a highly potent and selective leucine-rich repeat kinase 2 (LRRK2) inhibitor with K i and IC50 of 2 nM and 19 nM, respectively.
Targets
LRRK2 ; LRRK2 2 nM(Ki); 19 nM
In vitro
GNE-9605 is highly potent against LRRK2 in both biochemical (Ki = 2.0 nM) and cellular (IC50 = 19 nM) assays. In vitro human MDR1 permeability data, GNE-9605 exhibits excellent brain penetration in higher species.
In vivo
In vivo rat PK studies with GNE-9605 (1 mg/kg, p.o.) demonstrates a total plasma clearance of 26 mL/min/kg with excellent oral bioavailability (90%). In BAC transgenic mice expressing human LRRK2 protein with the G2019S Parkinson’s disease mutation, GNE-9605 (10 and 50 mg/kg, i.p.) inhibits in vivo LRRK2 Ser1292 autophosphorylation.
G2229072