C004019
Based on 1 Customer Validation
C004019 is a BBB-penetrable and small-molecule PROTAC that targets tau. C004019 can simultaneously recruit tau and E3 ligase, and effectively clear tau proteins by promoting the ubiquitination and proteasome-dependent degradation of tau, thereby improving synaptic and cognitive functions in Alzheimer's disease (AD) mice. C004019 can be used in the research of AD and tau protein-related diseases.
(Pink: Tau Protein ligand (HY-138679); Blue: VHL ligand (HY-138678); Black: linker (HY-140189)).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.72%
- No. CAS: 2417159-57-8
- Fòrmula: C49H70N12O9S2
- Peso molecular:1035.29
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Almacenamiento:
-20°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
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Actividad biológica
C004019 (0.01-100 μM; 24 h) does not cause significant changes in the viability of HEK293 cells stably expressing wild-type full-length human tau (HEK293-hTau)[1].
C004019 (0.01-20 μM; 24 h) inhibits the expression of total tau (Tau5) and phosphorylated tau in HEK293-hTau and SH-SY5Y cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293-hTau cells
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Concentration:0.01 μM, 0.1 μM, 1 μM, 10 μM and 20 μM
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Incubation Time:24 h
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Result:Induced a concentration-dependent reduction of total tau (Tau5) and tau phosphorylated (p-tau) at multiple AD-related sites (pS214, pS262, pS396, pS404).
C004019 (subcutaneous injection; 3-15 mg/kg; single dose) effectively clears tau protein in the brains of wild-type mice[1].
C004019 (subcutaneous injection; 3 mg/kg; once every 6 days for five times) promotes tau clearance and improves cognitive and synaptic functions in hTau and 3xTg-AD mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:hTau transgenic mice aged 12 months old[1]
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Dosage:3 mg/kg
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Administration:Subcutaneous injection (s.c.); once every 6 days for a total of 5 times
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Result:Significantly reduced total and p-tau levels in the hippocampal extracts.
Reduced both soluble and insoluble tau, more efficiently to the tau in the soluble fraction.
Ameliorated cognitive functions and dentritic plasticity in hTau transgenic mouse model.
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Animal Model:3xTg-AD mice aged 9.5 months old[1]
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Dosage:3 mg/kg
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Administration:Subcutaneous injection (s.c.); once every 6 days for a total of 5 times
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Result:Remarkably reduced both soluble and insoluble tau levels in hippocampal and cortex extracts, more efficiently to the tau in the soluble fraction.
Significantly reduced T22-positive tau in the soluble fraction.
Improved the cognitive and synaptic functions in 3xTg-AD mice.
Chemical Information
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No. CAS 2417159-57-8
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Appearance Solid
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Peso molecular 1035.29
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Fòrmula C49H70N12O9S2
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Color White to off-white
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SMILES
O=C(N1[C@H](C[C@@H](C1)O)C(NCC2=CC=C(C3=C(N=CS3)C)C=C2)=O)[C@H](C(C)(C)C)NC(COCCOCCOCCNC(CN(C4=NC(N5CCN(CCC5)C(C)=O)=NC(NCCC6=CC=CS6)=N4)C)=O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvente y solubilidad
DMSO : 50 mg/mL (48.30 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 | 0.9659 mL | 4.8296 mL | 9.6591 mL | 24.1478 mL |
| 5 mM | 0.1932 mL | 0.9659 mL | 1.9318 mL | 4.8296 mL | |
| 10 mM | 0.0966 mL | 0.4830 mL | 0.9659 mL | 2.4148 mL | |
| 15 mM | 0.0644 mL | 0.3220 mL | 0.6439 mL | 1.6099 mL | |
| 20 mM | 0.0483 mL | 0.2415 mL | 0.4830 mL | 1.2074 mL | |
| 25 mM | 0.0386 mL | 0.1932 mL | 0.3864 mL | 0.9659 mL | |
| 30 mM | 0.0322 mL | 0.1610 mL | 0.3220 mL | 0.8049 mL | |
| 40 mM | 0.0241 mL | 0.1207 mL | 0.2415 mL | 0.6037 mL |
C004019 Related Classifications
HY-138669 Related Classifications
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