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Verubecestat

Verubecestat (MK-8931) 是一种高亲和力的、具有口服活性的BACE1和BACE2抑制剂，Ki 分别为 2.2 nM 和 0.38 nM。它可以有效降低 Aβ40，并具有潜力用于阿尔茨海默氏病。

CAS号

1286770-55-5

分子式

C17H17F2N5O3S

主要靶点

BACE|Beta-Secretase

仅限科研使用

Cat No : CM06393

Print datasheet

Synonyms

维罗司他|MK-8931

验证数据展示

  • CAS No.: 1286770-55-5

    Verubecestat
    CAS#: 1286770-55-5

产品信息

Verubecestat (MK-8931) is an effective and specific β-secretase inhibitor and β-site APP-cleaving enzyme 1 inhibitor or BACE1 protein inhibitor.

CAS号 1286770-55-5
分子式 C17H17F2N5O3S
主要靶点 BACE|Beta-Secretase
主要通路 神经科学
分子量 409.41
纯度 99.49%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 维罗司他|MK-8931

靶点活性

BACE1:1.75 nM(Ki)|BACE2:0.37 nM(Ki)

体内活性

Verubecestat(MK-8931) dramatically lowers CSF and cortex Aβ40 in both rats and cynomolgus monkeys following a single oral dose. Due to the 20 h half-life of MK-8931 it is ideal for once-a-day dosing[2].

体外活性

Verubecestat(MK-8931) effectively reduces Aβ40 in cells with a Ki of 7.8 nM and an IC50 of 13 nM[2].

溶解度

DMSO:81 mg/mL (154.74 mM),Ethanol:5 mg/mL (9.55 mM),H2O:<1 mg/mL

参考文献

1.Evin G, et al. BioDrugs. 2016, 30(3):173-94.
2.Yan R, et al. Transl Neurodegener. 2016, 5:13.

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
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C1   V1   C2   V2