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NB-360

Names

[ CAS No. ]:
1262857-73-7

[ Name ]:
NB-360

Biological Activity

[Description]:

NB-360 is a potent, brain penetrable, and orally bioavailable dual BACE1/BACE2 inhibitor (IC50: mouse and human BACE1=5 nM; BACE2=6 nM). NB-360 shows a superior pharmacological profile and robust reduction of amyloid-β and neuroinflammation in amyloid precursor protein(APP) transgenic mice. NB-360 can completely block the progression of Aβ deposition in the brains of APP transgenic mice. NB-360 shows excellent selectivity over the related aspartyl proteases pepsin, cathepsin D and cathepsin E[1][2].

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> Beta-secretase

[Target]

IC50: 5 nM (Mouse and human BACE1), 6 nM (BACE2)[1]


[References]

[1]. Neumann U, et al. Mol Neurodegener. 2015 Sep 3;10:44. doi: 10.1186/s13024-015-0033-8.

[2]. Neumann U, et al. The β-secretase (BACE) inhibitor NB-360 in preclinical models: From amyloid-β reduction to downstream disease-relevant effects. Br J Pharmacol. 2019 Sep;176(18):3435-3446.

Chemical & Physical Properties

[ Molecular Formula ]:
C21H19F4N5O2

[ Molecular Weight ]:
449.40


Related Compounds