LY2886721, BACE-1 inhibitor

Description

MW 390.4 Da, Purity >98 %. Potent and selective BACE-1 inhibitor IC50 = 20.3 nM for recombinant hBACE-1 . Human BACE2 is inhibited with an IC50 of 10.2 nM. Does not inhibit other aspartyl proteases such as cathepsin D, pepsin, and renin. A potential agent to treat Alzheimers Disease. Inhibits production of Abeta in HEK-293 Swe cells IC50 values are 18.5 nM and 19.7 nM for Abeta1-40 and Abeta1-42 respectively and in PDAPP neuronal cells IC50 10 nM . Reduces dose-dependently brain levels of Abeta, C99 and sAPPbeta in orally administered mouse model and plasma Abeta in dog model. Ppenetrates the blood-brain barrier.