GNE-7915

一种选择性、可穿透脑屏障的LRRK2抑制剂（在生化和细胞基础实验中的Ki分别为2 nM和18.7 nM）；在携带人LRRK2蛋白G2019S帕金森病突变的BAC转基因小鼠中，抑制LRRK2 Ser1292的自磷酸化（体内IC50 = 20 nM）。A selective, brain-penetrable LRRK2 inhibitor (Kis = 2 and 18.7 nM in biochemical and cell-based assays, respectively); inhibits LRRK2 Ser1292 autophosphorylation in BAC transgenic mice expressing human LRRK2 protein with the G2019S Parkinson's disease mutation (IC50 = 20 nM in vivo).