Umibecestat
Based on 1 publication(s) in Google Scholar
Umibecestat (CNP520) is a beta-site amyloid precursor protein cleaving enzyme-1 (BACE-1) inhibitor with IC50s of 11 nM and 10 nM for human BACE-1 and mouse BACE-1, respectively. Umibecestat can be used for the research of alzheimer's disease.
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: 99.81%
- CAS 番号: 1387560-01-1
- 分子式: C19H15ClF7N5O2
- 分子量:513.80
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保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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
MedChemExpress（MCE）の使用を引用している文献 Umibecestat
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生物活性
IC50: 11 nM (human BACE-1), 10 nM (mouse BACE-1)[1]
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
3 nM
Compound: 5; CNP-520
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Inhibition of BACE1 in CHO cells expressing human APP assessed as reduction in amyloidbeta (1 to 40 residues) level incubated for 24 hrs by immunoassay method
Inhibition of BACE1 in CHO cells expressing human APP assessed as reduction in amyloidbeta (1 to 40 residues) level incubated for 24 hrs by immunoassay method
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[PMID: 30709653] |
Umibecestat (CNP520) is a potent BACE-1 inhibitor that is selective for BACE-1 over other human pepsin-like aspartic proteases, including BACE-2 and cathepsin D[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Umibecestat (CNP520) (3.1 mg/kg; oral administration; 7 days) shows a > 75% reduction on Aβ40 and Aβ42 in CSF after dosing and returns slowly to baseline over the next 7 days[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male rats (3-4 months old)[1]
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Dosage:1.5 mg/kg (3 μM/kg)-51.3 mg/kg (100 μM/kg)
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Administration:Given by oral gavage; 72 hours
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Result:Reduced 89.3±4.5% Aβ40 at the highest dose in brain tissue, and 50% lowering of rat brain Aβ40 (ED50) was 2.4±0.31 mg/kg. Reduced ~50% Aβ40 at a single oral 30 μM/kg (15.4 mg/kg) dose after 24 hours in both rat brain and CSF。
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Animal Model:3-month-old beagle dogs[1]
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Dosage:3.1 mg/kg (6 μM/kg)
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Administration:Oral administration; 7 days
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Result:Both Aβ40 and Aβ42 concentrations in CSF showed a > 75% reduction at 12-48 h after dosing and returned slowly to baseline over the next 7 days.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1387560-01-1
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性状 Solid
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分子量 513.80
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分子式 C19H15ClF7N5O2
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Color White to off-white
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SMILES
O=C(NC1=NC([C@@]2(CO[C@](C)(C(N)=N2)C(F)(F)F)C)=C(C=C1)F)C3=NC=C(C=C3Cl)C(F)(F)F
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別名
CNP520
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
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Journal Impact Factor
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Most Recent
溶剤 & 溶解度
DMSO : 100 mg/mL (194.63 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9463 mL | 9.7314 mL | 19.4628 mL | 48.6571 mL |
| 5 mM | 0.3893 mL | 1.9463 mL | 3.8926 mL | 9.7314 mL | |
| 10 mM | 0.1946 mL | 0.9731 mL | 1.9463 mL | 4.8657 mL | |
| 15 mM | 0.1298 mL | 0.6488 mL | 1.2975 mL | 3.2438 mL | |
| 20 mM | 0.0973 mL | 0.4866 mL | 0.9731 mL | 2.4329 mL | |
| 25 mM | 0.0779 mL | 0.3893 mL | 0.7785 mL | 1.9463 mL | |
| 30 mM | 0.0649 mL | 0.3244 mL | 0.6488 mL | 1.6219 mL | |
| 40 mM | 0.0487 mL | 0.2433 mL | 0.4866 mL | 1.2164 mL | |
| 50 mM | 0.0389 mL | 0.1946 mL | 0.3893 mL | 0.9731 mL | |
| 60 mM | 0.0324 mL | 0.1622 mL | 0.3244 mL | 0.8110 mL | |
| 80 mM | 0.0243 mL | 0.1216 mL | 0.2433 mL | 0.6082 mL | |
| 100 mM | 0.0195 mL | 0.0973 mL | 0.1946 mL | 0.4866 mL |
Umibecestat 関連分類
HY-119689 関連分類
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