| Identification | Back Directory | [Name]
Atabecestat | [CAS]
1200493-78-2 | [Synonyms]
Atabecestat
JNJ-54861911
Atabecestat (JNJ-54861911)
2-Pyridinecarboxamide, N-[3-[(4S)-2-amino-4-methyl-4H-1,3-thiazin-4-yl]-4-fluorophenyl]-5-cyano- | [Molecular Formula]
C18H14FN5OS | [MDL Number]
MFCD31631590 | [MOL File]
1200493-78-2.mol | [Molecular Weight]
367.4 |
| Hazard Information | Back Directory | [Uses]
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: | 5-week-old APPPS1 mice[2] | | Dosage: | 100 and 300 mg/kg | | Administration: | Oral gavage; 100 and 300 mg/kg; once daily for 3 days | | Result: | Reduced the level of human Aβ1-40 and Aβ1-42 levels in the brain of APPPS1 mice at a dose of 300 mg/kg and resulted in less reduction of human Aβ levels at 24 h with a dose of 100 mg/kg.
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| [IC 50]
BACE1 | [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. DOI:10.1016/j.trci.2016.08.001
[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. DOI:10.1016/j.nbd.2021.105365 |
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| Company Name: |
cjbscvictory
|
| Tel: |
13348960310 13348960310; |
| Website: |
https://www.weikeqi-biotech.com/ |
| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
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