GNE0877 is a highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitor with an IC50 of 3 nM.
GNE0877 is a potent, orally active, and brain-penetrable inhibitor of LRRK2, showcasing an IC50 of 3 nM and a Ki of 0.7 nM, marking its potential for neuroscience research[1].
体内研究
Furthermore, when administered intraperitoneally at doses of 10 and 50 mg/kg in a single dose, GNE0877 effectively inhibits LRRK2 Ser1292 autophosphorylation[1].
体外研究
In cellular assays, GNE0877 demonstrates strong potency within human liver microsomes and hepatocytes at a concentration of 1 μM over a time frame of 10-30 minutes[1].
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