| Description | 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 在APP基因转基因小鼠的脑部阻止了Aβ沉积的进展，可用于制造淀粉样病理模型。NB-360 在大鼠和犬类中也实现了Aβ的大量减少。此外，NB-360中断了在APP基因转基因小鼠脑部的激活炎症细胞的积累。NB-360长期治疗APP基因转基因小鼠后，动物出现了灰白色毛发斑块[2]。 |
| Target activity | BACE1 (mouse , human):5 nM , BACE2:6 nM |
| molecular weight | 449.4 |
| Molecular formula | C21H19F4N5O2 |
| CAS | 1262857-73-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 45 mg/mL (100.13 mM) |
| 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. |