| Description | AZD3839 free base is a potent and selective BACE1 inhibitor with Ki of 26.1 nM, about 14-fold selectivity over BACE2. Phase 1. |
| In vitro | 在SH-SY5Y细胞中，AZD3839高效降低Aβ40水平，IC50为4.8 nM，且降低sAPPβ形成，IC50为16.7 nM。AZD3839同样有效降低来自C57BL/6小鼠初级皮层神经元、N2A细胞和Dunkin-Hartley豚鼠初级皮层神经元分泌的Aβ40水平，IC50值分别为50.9、32.2和24.8 nM。[1] AZD3839在细胞实验中通过抑制BACE1活性达到上述效果，其IC50值为16.7 nM。[2] |
| In vivo | 在C57BL/6小鼠中，AZD3839（69 mg/kg，口服）呈剂量和时间依赖性降低血浆和大脑Aβ。在豚鼠和非人灵长类动物中，AZD3839同样抑制Aβ生成。[1] |
| Target activity | BACE1:26.1 nM(Ki) |
| Synonyms | AZD3839 |
| molecular weight | 431.41 |
| Molecular formula | C24H16F3N5 |
| CAS | 1227163-84-9 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 80 mg/mL (185.4 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: 80 mg/mL (185.4 mM) |
| References | 1. Jeppsson F, et al. J Biol Chem. 2012, 287(49), 41245-41257. 2. Swahn BM, et al. J Med Chem. 2012, 55(21), 9346-9361. |