LY450139(Semagacestat)

英文名 ：≥98%(HPLC)

库存 ：50

CAS号 ：425386-60-3

规格 ：5mg/25mg/100mg

一种有效的γ-分泌酶抑制剂，作用于Aβ42，Aβ40和Aβ38，IC50分别为10.9nM、12nM和12.1nM。LY450139 is an inhibitor of the γ-secretase complex. It causes a reduction in the secretion of Aβ42, Aβ40 and Aβ38 from H4 human glioma cells stably overexpressing human wild-type APP into the culture medium. Semagacestat increases β-CTF in cell lysates, and the increase can be attenuated at high concentrations. Semagacestat inhibits Notch signaling with IC50 of 14.1 nM, and shows minimal Notch-sparing selectivity with Notch IC50/Aβ42 IC50 only 1.3. Semagacestat causes a concentration-dependent decrease in Aβ40 secreted into the medium with IC50 of 111 nM from murine CTX expressing endogenous murine APP, but murine Aβ42 formation in CTX is roughly 12-fold less than Aβ40 in accordance with data for neurons from wild type mice。