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编 号:F754509
分子式:C21H31N5OS
分子量:401.57
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生物活性:
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.

体内研究:
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).

体外研究:
BACE1/2-IN-1 (compound 34) demonstrates slight selectivity for BACE2 and retained >3000 fold selectivity against Cathepsin D.
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