Bioactivity | Atabecestat (JNJ-54861911) is a potent brain-penetrant and orally active β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor, achieves robust and high CSF Aβ reduction. Atabecestat s tolerated and displays a sustained pharmacokinetic (PK) and pharmacodynamic (PD) characteristics. Atabecestat has the potential for Alzheimer's Disease treatment[1]. | ||||||||||||
In Vivo | Atabecestat (100 and 300 mg/kg; p.o. once daily for 3 days) reduces the human Aβ levels in mice[2].Atabecestat (300 mg/kg; p.o. once) inhibits the exacerbation of vascular abnormalities in APPPS1 mice with 3D6 treatment[2]. Animal Model: | ||||||||||||
Name | Atabecestat | ||||||||||||
CAS | 1200493-78-2 | ||||||||||||
Formula | C18H14FN5OS | ||||||||||||
Molar Mass | 367.40 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [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. |