β-Secretase Inhibitor IV

BACE1和2的抑制剂（对人类BACE1和2的IC50分别为15和230nM）；对BACE1和2的选择性比对天冬氨酰蛋白酶肾素和组织蛋白酶D的选择性高500倍以上；抑制转染了截短人类APP的HEK293T细胞中APP的分泌（IC50分别为29nM）；抑制原代鸡神经元中Aβ肽Aβ38、Aβ40和Aβ42的形成（IC50分别为3.7、4.7和4.8nM）。An inhibitor of BACE1 and 2 (IC50s = 15 and 230 nM for human BACE1 and 2, respectively); has >500-fold selectivity for BACE1 and 2 over the aspartyl proteases renin and cathepsin D; inhibits secretion of APP (IC50 = 29 nM) in HEK293T cells transfected with a truncated human APP; inhibits formation of the Aβ peptides Aβ38, Aβ40, and Aβ42 in primary chick neurons (IC50s = 3.7, 4.7, and 4.8 nM, respectively).