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AZD 3293 is an inhibitor of β-secretase 1 (BACE1) and BACE2 (Kis = 0.4 and 0.8 nM, respectively).1 It is selective for BACE1 and BACE2 over cathepsin D, γ-secretase, and human-ether-a-go-go (hERG; IC50s = 3,797, >25,000, and 4,700 nM, respectively). AZD 3293 inhibits the secretion of amyloid-β (1-40) (Aβ40) in primary mouse and guinea pig neuronal cultures (IC50s = 0.61 and 0.31 NM, respectively), as well as in SH-SY5Y cells overexpressing human amyloid precursor protein (APP; IC50 = 0.08 nM). In vivo, AZD 3293 (50, 100, and 200 µmol/kg) reduces plasma and brain levels of Aβ40 and brain levels of Aβ42 in mice.
WARNING This product is not for human or veterinary use.
1. AZD3293: A novel, orally active BACE1 inhibitor with high potency and permeability and markedly slow off-