NB-360 是一种有效的脑穿透性 BACE1 和 BACE2 抑制剂,对小鼠和人源 BACE1 和 BACE2 的 IC50 分别为 5、5 和 6 nM。 NB-360 对相关的天冬氨酰蛋白酶、胃蛋白酶、组织蛋白酶 E 和组织蛋白酶 D 具有出色的特异性。
产品描述
NB-360 is a potent and brain-penetrable inhibitor of BACE1 and BACE2 with IC50s of 5, 5, and 6 nM for mouse and human BACE1 and BACE2. NB-360 exhibits excellent selectivity over the related aspartyl proteases pepsin, cathepsin E, and cathepsin D.
体内活性
NB-360 blocks the progression of Aβ deposition in the brains of APP transgenic mice, a model for amyloid pathology. Almost complete reduction of Aβ was achieved also in rats and in dogs. NB-360 stops accumulation of activated inflammatory cells in the brains of APP transgenic mice. Upon chronic treatment of APP transgenic mice, patches of grey hairs appeared[2].
Cas No.
1262857-73-7
分子式
C21H19F4N5O2
分子量
449.4
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years