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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.97%
- CAS 番号: 1200493-78-2
- 分子式: C18H14FN5OS
- 分子量:367.40
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 Atabecestat
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生物活性
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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 |
化学情報
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CAS 番号 1200493-78-2
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性状 Solid
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分子量 367.40
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分子式 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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別名
JNJ-54861911
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
[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 |
Atabecestat 関連分類
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