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LY2811376 is the first orally available non-peptidic BACE1 inhibitor that produces profound Aβ-lowering effects in animals. LY2811376 has 10-fold selectivity towards BACE1 over BACE2, and more than 50-fold inhibition over other aspartic proteases including cathepsin D, pepsin, or renin. LY2811376 inhibits Aβ secretion with EC50 of ~100 nM in primary neuronal cultures of PDAPP transgenic mouse. Administration of LY2811376 (10, 30 and 100 mg/kg doses) results in dose-dependent, significant reductions in Aβ, as well as sAPPβ and C99. LY2811376 treatment yields a concentration-dependent decrease in Aβ secretion in APP-overexpressing HEK293 cells.
Small Structures. 2024 Jul 05;25(7):3693.
A Bilingual Nanobiosensor for Cross-Category Integrated Decoding of the Beta-Site Amyloid Precursor Protein-Cleaving Enzyme 1–Aβ Oligomer Signaling Pathway
LY2811376 purchased from AbMole
| Molecular Weight | 320.36 |
| Formula | C15H14F2N4S |
| CAS Number | 1194044-20-6 |
| Solubility (25°C) | Ethanol 48 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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