| Description | Atabecestat (JNJ-54861911) is an orally active and brain-permeable inhibitor of β-site amyloid precursor protein cleaving enzyme 1 (BACE1) that slows cognitive decline in participants with preclinical Alzheimer's disease.Atabecestat is used in the study of Alzheimer's disease. |
| In vivo | 在 5 周大的 APPPS1 小鼠中，Atabecestat（100和300 mg/kg；口服灌注；100 和 300 mg/kg；每日一次，连续 3 天）能够在 300 mg/kg的剂量下降低 APPPS1 小鼠大脑中人类 Aβ1-40 和Aβ1-42 水平，并在 100 mg/kg 的剂量下导致 24 小时内人类 Aβ 水平的减少较少[2]。 |
| Synonyms | RSC-385896, JNJ-54861911 |
| molecular weight | 367.4 |
| Molecular formula | C18H14FN5OS |
| CAS | 1200493-78-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 200 mg/mL (544.37 mM), Sonication is recommended. |
| References | 1. Timmers M, et al. Profiling the dynamics of CSF and plasma Aβ reduction after treatment with JNJ-54861911, a potent oral BACE inhibitor.Alzheimers Dement (N Y). 2016 Aug 24;2(3):202-212. 2. Janssens J, et al. Passive immunotherapy with a novel antibody against 3pE-modified Aβ demonstrates potential for enhanced efficacy and favorable safety in combination with BACE inhibitor treatment in plaque-depositing mice. Neurobiol Dis. 2021 Jul;154:105365. |