Atabecestat
Based on 1 publication(s) in Google Scholar
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.97%
- No. CAS: 1200493-78-2
- Fòrmula: C18H14FN5OS
- Peso molecular:367.40
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Atabecestat
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Actividad biológica
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BACE1 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:5-week-old APPPS1 mice[2]
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Dosage:100 and 300 mg/kg
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Administration:Oral gavage; 100 and 300 mg/kg; once daily for 3 days
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1200493-78-2
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Appearance Solid
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Peso molecular 367.40
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Fòrmula C18H14FN5OS
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Color White to off-white
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SMILES
O=C(C1=NC=C(C#N)C=C1)NC2=CC=C(F)C([C@@]3(C)N=C(N)SC=C3)=C2
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Synonyms
JNJ-54861911
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
Solvente y solubilidad
DMSO : 250 mg/mL (680.46 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (272 KB)
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SDS (418 KB)
- English - EN (418 KB)
- Français - FR (418 KB)
- Deutsch - DE (418 KB)
- Norwegian - NO (418 KB)
- Español - ES (418 KB)
- Swedish - SV (418 KB)
- Italian - IT (418 KB)
- Korean - KR (418 KB)
- Portuguese - PT (418 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7218 mL | 13.6091 mL | 27.2183 mL | 68.0457 mL |
| 5 mM | 0.5444 mL | 2.7218 mL | 5.4437 mL | 13.6091 mL | |
| 10 mM | 0.2722 mL | 1.3609 mL | 2.7218 mL | 6.8046 mL | |
| 15 mM | 0.1815 mL | 0.9073 mL | 1.8146 mL | 4.5364 mL | |
| 20 mM | 0.1361 mL | 0.6805 mL | 1.3609 mL | 3.4023 mL | |
| 25 mM | 0.1089 mL | 0.5444 mL | 1.0887 mL | 2.7218 mL | |
| 30 mM | 0.0907 mL | 0.4536 mL | 0.9073 mL | 2.2682 mL | |
| 40 mM | 0.0680 mL | 0.3402 mL | 0.6805 mL | 1.7011 mL | |
| 50 mM | 0.0544 mL | 0.2722 mL | 0.5444 mL | 1.3609 mL | |
| 60 mM | 0.0454 mL | 0.2268 mL | 0.4536 mL | 1.1341 mL | |
| 80 mM | 0.0340 mL | 0.1701 mL | 0.3402 mL | 0.8506 mL | |
| 100 mM | 0.0272 mL | 0.1361 mL | 0.2722 mL | 0.6805 mL |
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