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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.81%
- No. CAS: 1387560-01-1
- Fòrmula: C19H15ClF7N5O2
- Peso molecular:513.80
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Almacenamiento:
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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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
Publications Citing Use of MedChemExpress (MCE) Umibecestat
More
Actividad biológica
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 |
|---|---|---|---|---|
| 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
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1387560-01-1
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Appearance Solid
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Peso molecular 513.80
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Fòrmula 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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Synonyms
CNP520
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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
Solvente y solubilidad
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (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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Instrucciones de manejo (2659 KB)
Referencias
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 Related Classifications
HY-119689 Related Classifications
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