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Umibecestat (CNP520) is a beta-site amyloid precursor protein cleaving enzyme-1 (BACE-1) inhibitor with IC 50 s of 11 nM and 10 nM for human BACE-1 and mouse BACE-1, respectively Umibecestat can be used for the research of alzheimer's disease. In Vitro Umibecestat (CNP520) is a potent BACE-1 inhibitor that is selective for BACE-1 over other human pepsin-like aspartic proteases, including BACE-2 and cathepsin D. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo Umibecestat (CNP520) (1.5-51.3 mg/kg; given by oral gavage; 72 hours) shows a dose-dependent effects on Aβ40 and a long duration of action in both rat brain and CSF . Umibecestat (CNP520) (3.1 mg/kg; oral administration; 7 days) shows a > 75% reduction on Aβ40 and Aβ42 in CSF after dosing and returns slowly to baseline over the next 7 days . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male rats (3-4 months old) Dosage: 1.5 mg/kg (3 μM/kg)-51.3 mg/kg (100 μM/kg) Administration: Given by oral gavage; 72 hours Result: Reduced 89.3±4.5% Aβ40 at the highest dose in brain tissue, and 50% lowering of rat brain Aβ40 (ED50) was 2.4±0.31 mg/kg. Reduced ~50% Aβ40 at a single oral 30 μM/kg (15.4 mg/kg) dose after 24 hours in both rat brain and CSF。 Animal Model: 3-month-old beagle dogs Dosage: 3.1 mg/kg (6 μM/kg) Administration: Oral administration; 7 days Result: Both Aβ40 and Aβ42 concentrations in CSF showed a > 75% reduction at 12-48 h after dosing and returned slowly to baseline over the next 7 days. Form:Solid IC50& Target:IC50: 11 nM (human BACE-1), 10 nM (mouse BACE-1)
中文名称
Umibecestat
英文名称
Umibecestat
中文别名
乌米贝司他
英文别名
1387560-01-1 | US8637508, 34 | SCHEMBL10382672 | Umibecestat | WHO 10872 | 6,7-Dihydro-1,2,3,10-tetramethoxy-7-(methylamino)-benzo(alpha)heptalen-9(5H)-one | 2-Pyridinecarboxamide, N-(6-((3R,6R)-5-amino-3,6-dihydro-3,6-dimethyl-6-(trifluoromethyl)-2H-1,4-
CAS号
1387560-01-1
分子式
C19H15ClF7N5O2
分子量
513.80 g/mol
精确质量
≥99%
PSA
102.000 Ų
Logp
2.900
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Umibecestat 5mg

品牌:阿拉丁
货号:U646410-5mg
级别: ≥99%
货期:30天
已售 976 件
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5mg

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