PROTAC α-Synuclein/Tau degrader 1
Based on 1 Customer Validation
PROTAC α-Synuclein/Tau degrader 1 is a blood-brain barrier-penetrant dual PROTAC degrader of α-synuclein (α-Syn) and tau, with DC50 of 1.57 μM and 4.09 μM, respectively. PROTAC α-Synuclein/Tau degrader 1 binds to α-Syn and tau PFF, with KDs of 0.47 and 2.78 μM, respectively. PROTAC α-Synuclein/Tau degrader 1 exhibits degradation effect mediated by the ubiquitin-proteasome system (UPS). PROTAC α-Synuclein/Tau degrader 6 can be used for the study of Parkinson’s disease (PD) (Pink: α-Synuclein/Tau ligand (HY-151035); Blue: CRBN ligase ligand (HY-14658); Black: Linker (HY-128803)).
(Pink: Tau Protein and α-synuclein ligand (HY-151035); Blue: Cereblon ligand (HY-14658); Black: linker (HY-128803)).
For research use only. We do not sell to patients.
- Purity: 99.28%
- CAS No.: 3032208-24-2
- Formula: C37H39N5O9S
- Molecular Weight:729.80
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Bioactive Compound Library Max
HY-L181
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Bioactive Compound Library
HY-L001
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Neuronal Signaling Compound Library
HY-L013
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CNS-Penetrant Compound Library
HY-L028
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Anti-Parkinson's Disease Compound Library
HY-L085
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Neurodegenerative Disease-related Compound Library
HY-L086
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PROTAC Library
HY-L151
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Extracellular Vesicles (EVs) Compound Library
HY-L168
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Multi-Target Compound Library
HY-L176
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MCE Bioactive Compound Library
HY-L001V
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High-Throughput Bioactive Compound Library
HY-L205
Biological Activity
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α-synuclein 1.57 μM (DC50) |
Cereblon |
PROTAC α-Synuclein/Tau degrader 1 (Compound T4) (5 μM, 24 h) inhibit the α-Syn aggregate-mediated ROS generation and ΔΨm loss and protect SH-SY5Y Cells from α-Syn aggregate-associated toxicity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
PROTAC α-Synuclein/Tau degrader 1 (8 mg/kg, i.v., single dose) shows good half-life in both plasma (AUC0-24h = 109.21 μM·h, t1/2 = 3.24 h) and brain tissues (AUC0-24h = 6.02 μM·h, t1/2 = 4.21 h) in C57BL/6 mice and the absorption, distribution, metabolism, and excretion (ADME) properties in SD rats are basically consistent[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MPTP (HY-15608)-induced PD model established in Male C57BL/6 mice (60-70 days old, weighed 22-24 g) [1]
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Dosage:2, 4, and 8 mg/kg
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Administration:Intravenous injection (i.v.), once daily for 7 days
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Result:Significantly reduced midbrain α-Syn aggregates (reduced by 78%) and total tau in the hippocampus (decreased by 61%).
Reduced the area of α-Syn-positive cells in the SNc region by 72%.
Increased the survival rate of dopamine neurons by 65%.
No abnormalities at 8 mg/kg and only a slight increase in ALT/AST was observed at 80 mg/kg.
Chemical Information
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CAS No. 3032208-24-2
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Appearance Solid
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Molecular Weight 729.80
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Formula C37H39N5O9S
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Color Light yellow to yellow
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SMILES
O=C(N1C2C(NC(CC2)=O)=O)C3=CC=CC(OCC(NCCOCCOCCOCCNC4=CC=C(C(S5)=NC6=C5C=C(C)C=C6)C=C4)=O)=C3C1=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (137.02 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. 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. 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)
Purity & Documentation
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Data Sheet (275 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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Handling Instructions (2659 KB)
References
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. 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 |
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| DMSO | 1 mM | 1.3702 mL | 6.8512 mL | 13.7024 mL | 34.2560 mL |
| 5 mM | 0.2740 mL | 1.3702 mL | 2.7405 mL | 6.8512 mL | |
| 10 mM | 0.1370 mL | 0.6851 mL | 1.3702 mL | 3.4256 mL | |
| 15 mM | 0.0913 mL | 0.4567 mL | 0.9135 mL | 2.2837 mL | |
| 20 mM | 0.0685 mL | 0.3426 mL | 0.6851 mL | 1.7128 mL | |
| 25 mM | 0.0548 mL | 0.2740 mL | 0.5481 mL | 1.3702 mL | |
| 30 mM | 0.0457 mL | 0.2284 mL | 0.4567 mL | 1.1419 mL | |
| 40 mM | 0.0343 mL | 0.1713 mL | 0.3426 mL | 0.8564 mL | |
| 50 mM | 0.0274 mL | 0.1370 mL | 0.2740 mL | 0.6851 mL | |
| 60 mM | 0.0228 mL | 0.1142 mL | 0.2284 mL | 0.5709 mL | |
| 80 mM | 0.0171 mL | 0.0856 mL | 0.1713 mL | 0.4282 mL | |
| 100 mM | 0.0137 mL | 0.0685 mL | 0.1370 mL | 0.3426 mL |
PROTAC α-Synuclein/Tau degrader 1 Related Classifications
HY-157839 Related Classifications
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