NB-360

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

NB-360 是一种有效的脑渗透性 BACE1 和 BACE2 抑制剂，对小鼠和人类 BACE1 和 BACE2 的 IC50 分别为 5、5 和 6 nM。 NB-360 比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 表现出优异的选择性。

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.(In Vivo):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.

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Metabolic Enzyme/Protease

BACE

Lp-PLA2

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1262857-73-7

449.41

C21H19F4N5O2

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (556.30 mM)

Cc1cc(cnc1C(=O)Nc1ccc(F)c(c1)[C@]1(C)CO[C@](C)(C(N)=N1)C(F)(F)F)C#N

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(-20℃)

With Ice Pack

≥ 2 years