| Description | Verubecestat (MK-8931) (MK-8931) is an effective and specific β-secretase inhibitor and β-site APP-cleaving enzyme 1 inhibitor or BACE1 protein inhibitor. |
| In vitro | Verubecestat(MK-8931) 在细胞中有效降低Aβ40，其Ki值为7.8 nM，IC50值为13 nM[2]。 |
| In vivo | Verubecestat(MK-8931)通过单次口服显著降低大鼠和猕猴的脑脊液和大脑皮层中的Aβ40水平。鉴于MK-8931的半衰期为20小时，它非常适合每天一次的给药方式[2]。 |
| Target activity | BACE1:1.75 nM(Ki), BACE2:0.37 nM(Ki) |
| Synonyms | MK-8931, 维罗司他 |
| molecular weight | 409.41 |
| Molecular formula | C17H17F2N5O3S |
| CAS | 1286770-55-5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: 5 mg/mL (9.55 mM) DMSO: 81 mg/mL (154.74 mM) |
| References | 1. Evin G, et al. BioDrugs. 2016, 30(3):173-94. 2. Yan R, et al. Transl Neurodegener. 2016, 5:13. |