Lanabecestat (AZD-3293, LY-3314814) is a potent, orally active and brain-permeable BACE1 inhibitor with Ki of 0.4 nM.
Lanabecestat (AZD-3293, LY-3314814) shows equipotency against hBACE2 (Ki=0.8 nM), >25,000- and >41,000-fold selectivity against cathepsin D and γ-secretase。
Lanabecestat (AZD-3293, LY-3314814) significantly reduces Aβ40, Aβ42, and sAβPPβ in mouse, guinea pig and dog, also shows in vitro potency in mouse and guinea pig primary cortical neuronal cells (IC50<1 nM)。
Lanabecestat (AZD-3293, LY-3314814) reduces cerebrospinal fluid (CSF) Aβ1-40 and Aβ1-42 in clinical trails.
