Atabecestat
Atabecestat Basic information
- Product Name:
- Atabecestat
- 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-
- (S)-N-(3-(2-Amino-4-methyl-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-cyanopicolinamide
- CAS:
- 1200493-78-2
- MF:
- C18H14FN5OS
- MW:
- 367.4
- Mol File:
- 1200493-78-2.mol
Atabecestat Chemical Properties
- Density
- 1.39±0.1 g/cm3(Predicted)
- pka
- 9.90±0.70(Predicted)
- form
- Solid
- color
- White to off-white
Atabecestat Usage And Synthesis
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. |
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
AtabecestatSupplier
- Tel
- 021-52996696，15000506266 15000506266
- Tel
- 021-65675885 18964387627
- info@efebio.com
- Tel
- 021-31433387 15618786686
- sales@rechemscience.com
- Tel
- +86 18721201413
- sales@biopharmaleader.com
- Tel
- +1-781-999-5354; +17819995354
- marketing@targetmol.com