| Description |
BACE1/2-IN-1 (compound 34) is a potent BACE1 and BACE2 inhibitor, with an IC50 of 0.01 and 0.0053 μM, respectively. BACE1/2-IN-1 shows a combination of lower Pgp efflux ratio and improved passive permeability. BACE1/2-IN-1 displays reduced liver microsomal metabolic stability[1].
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| Related Catalog |
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| Target |
IC50: 0.0053 μM (BACE2), 0.01 μM (BACE1), 160 μM (Cathepsin D)[1]
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| In Vitro |
BACE1/2-IN-1 (compound 34) demonstrates slight selectivity for BACE2 and retained >3000 fold selectivity against Cathepsin D[1].
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| In Vivo |
BACE1/2-IN-1 (compound 34) (PDAPP (V717F) transgenic mice, 0-100 mg/kg, Subcutaneous injection, once) shows significant reduction in PDAPP mouse cortex Aβ at 100 mg/kg (40%), and 30 mg/kg (24%), but not at 10 mg/kg (12%NS)[1].
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| References |
[1]. Winneroski LL, et al. Preparation and biological evaluation of BACE1 inhibitors: Leveraging trans-cyclopropyl moieties as ligand efficient conformational constraints. Bioorg Med Chem. 2020 Jan 1;28(1):115194.
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