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CAS No.: 1286770-55-5

Verubecestat/维罗司他 Catalog No. CSN18740

Synonyms: MK-8931;MK-8931 Free Base;MK-8931-009

Verubecestat is a BACE1 inhibitor. MK-8931 binds significantly to β-secretase.

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技术信息

生物活性

描述β-secretase 1 (BACE1) was discovered to initiate the cleavage of amyloid precursor protein (APP) at the β-secretase site. Only after this cleavage does γ-secretase further cleave the BACE1-cleaved C-terminal APP fragment to release Aβ which is the potential cause of Alzheimer's disease (AD)^[3]. Verubecestat (MK-8931) is a potent, selective, structurally unique BACE1 inhibitor that reduced plasma, cerebrospinal fluid (CSF), and brain concentrations of Aβ40, Aβ42, and sAPPβ (a direct product of BACE1 enzymatic activity) after acute and chronic administration to rats and monkeys. Chronic treatment of rats and monkeys with verubecestat achieved exposures >40-fold higher than those being tested in clinical trials in AD patients yet did not elicit many of the adverse effects previously attributed to BACE inhibition^[4].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01537757	Alzheimer's Disease	Phase 1	Completed	-	-
NCT01496170	Alzheimer's Disease	Phase 1	Completed	-	-
NCT01953601	Amnestic Mild Cognitive Impair... more >>ment Alzheimer's Disease Prodromal Alzheimer's Disease Collapse <<	Phase 3	Terminated	-	-

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参考文献

[1] Yan R. Stepping closer to treating Alzheimer's disease patients with BACE1 inhibitor drugs. Transl Neurodegener. 2016 Jul 14;5:13.
[2] Nisha CM, Kumar A, et al. Molecular Docking and In Silico ADMET Study Reveals Acylguanidine 7a as a Potential Inhibitor of β-Secretase. Adv Bioinformatics. 2016;2016:9258578.
[3] O'Brien RJ, Wong PC. Amyloid precursor protein processing and Alzheimer's disease. Annu Rev Neurosci. 2011;34:185-204.
[4] Kennedy ME, Stamford AW, Chen X, et al. The BACE1 inhibitor verubecestat (MK-8931) reduces CNS β-amyloid in animal models and in Alzheimer's disease patients. Sci Transl Med. 2016;8(363):363ra150.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4425 mL
- 12.2127 mL
- 24.4254 mL
- 5 mM
- 0.4885 mL
- 2.4425 mL
- 4.8851 mL
- 10 mM
- 0.2443 mL
- 1.2213 mL
- 2.4425 mL

技术信息

CAS号

1286770-55-5

储存条件

粉末: Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H17F2N5O3S

运输

蓝冰

分子量

409.41

别名

MK-8931;MK-8931 Free Base;MK-8931-009;SCH-900931;维罗司他

溶解度

DMSO	66.67 mg/mL (162.8 mM)
Water	insoluble

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