VerubeceSTAT 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。
产品描述
Verubecestat (MK-8931) is an effective and specific β-secretase inhibitor and β-site APP-cleaving enzyme 1 inhibitor or BACE1 protein inhibitor.
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].
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].
Cas No.
1286770-55-5
分子式
C19H18F5N5O5S
分子量
523.43
别名
MK-8931;维罗司他
储存和溶解度
H2O:<1 mgml
Ethanol:5 mg/mL (9.55 mM)
DMSO:81 mg/mL (154.74 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
