| Bioactivity | 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]. | ||||||||||||
| Target | IC50: 5 nM (Mouse and human BACE1), 6 nM (BACE2) | ||||||||||||
| Name | NB-360 | ||||||||||||
| CAS | 1262857-73-7 | ||||||||||||
| Formula | C21H19F4N5O2 | ||||||||||||
| Molar Mass | 449.40 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |
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.
