PF-06751979 is an inhibitor of β-site amyloid precursor protein cleaving enzyme 1 (BACE1) (IC50 of 7.3 nM in BACE1 binding assay).

PF-06751979 shows improved selectivity over BACE2 (IC50=194 nM) in binding (27-fold) relative to the literature examples and across multiple chemical series in BACE1 program.

PF-06751979 displays excellent brain penetration, potent in vivo efficacy, and broad selectivity over related aspartyl proteases including BACE2. Acute administration of PF-06751979 yields a robust dose-responsive and time-dependent reduction of cerebral spinal fluid (CSF) Aβx-40 with peak inhibition at 3 h of >77%.[1].

1818339-66-0

C18H19F2N5O3S2

455.5

Ethanol:50 mg/mL (109.77 mM),Need ultrasonic
DMSO:150 mg/mL (329.31 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years