PROTAC α-synuclein degrader 5
Based on 1 Customer Validation
PROTAC α-synuclein degrader 5 is a highly selective small-molecule degrader (PROTAC) of α-synuclein aggregates, with a DC50 of 7.51 μM and the highest degradation rate Dmax of 89%. PROTAC α-synuclein degrader 5 contains probe molecule sery308 and E3 ligase ligands. PROTAC α-synuclein degrader 5 can be used for neurological disease research.
For research use only. We do not sell to patients.
- Purity: 99.80%
- CAS No.: 2781922-42-5
- Formula: C39H41N7O10
- Molecular Weight:767.78
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Storage:
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Biological Activity
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α-synuclein Aggregation |
PROTAC α-synuclein degrader 5 (Compound 2b) (0-40 μM, 48 hour) decreases the level of α-synuclein aggregates within the treatment period in preformed fibril (PFF) -seeding model cells[1].
PROTAC α-synuclein degrader 5 (0-10 μM, 48 hour) degrades α-synuclein aggregates in a dose-dependent manner, as indicated by the reduced number and density of α-synuclein (+) punctate as well as the gradually declined fluorescence intensity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Preformed fibril (PFF)-seeding model in HEK-293T cells
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Concentration:0-40 μM
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Incubation Time:0-48 hours
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Result:Decreased the level of α-synuclein aggregates within the treatment period. This kind of change became statistically significant by 3h and reached its plateau after 24h.
Lowered the level of α-synuclein aggregates in model cells after treatment of 48 h.
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Cell Line:HEK-293T cells
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Concentration:0-10 μM
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Incubation Time:48 hours
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Result:Degraded α-synuclein aggregates inadose-dependent manner, as indicated bythe reduced number and density of α-synuclein (+) punctae aswell asthe gradually declined fluorescence intensity.
Chemical Information
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CAS No. 2781922-42-5
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Appearance Solid
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Molecular Weight 767.78
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Formula C39H41N7O10
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Color Light yellow to yellow
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SMILES
O=C(NCCOCCOCCOCCNC1=CC=CC(C(N2C3C(NC(CC3)=O)=O)=O)=C1C2=O)CNC4=CC(C5=CC(C6=CC7=C(C=C6)OCO7)=NN5)=CC=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
DMSO : ≥ 100 mg/mL (130.25 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (sealed storage, away from moisture and 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 (sealed storage, away from moisture and 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)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3.75 mg/mL (4.88 mM); Clear solution
This protocol yields a clear solution of ≥ 3.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (271 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 (sealed storage, away from moisture and 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 | 1.3025 mL | 6.5123 mL | 13.0246 mL | 32.5614 mL |
| 5 mM | 0.2605 mL | 1.3025 mL | 2.6049 mL | 6.5123 mL | |
| 10 mM | 0.1302 mL | 0.6512 mL | 1.3025 mL | 3.2561 mL | |
| 15 mM | 0.0868 mL | 0.4342 mL | 0.8683 mL | 2.1708 mL | |
| 20 mM | 0.0651 mL | 0.3256 mL | 0.6512 mL | 1.6281 mL | |
| 25 mM | 0.0521 mL | 0.2605 mL | 0.5210 mL | 1.3025 mL | |
| 30 mM | 0.0434 mL | 0.2171 mL | 0.4342 mL | 1.0854 mL | |
| 40 mM | 0.0326 mL | 0.1628 mL | 0.3256 mL | 0.8140 mL | |
| 50 mM | 0.0260 mL | 0.1302 mL | 0.2605 mL | 0.6512 mL | |
| 60 mM | 0.0217 mL | 0.1085 mL | 0.2171 mL | 0.5427 mL | |
| 80 mM | 0.0163 mL | 0.0814 mL | 0.1628 mL | 0.4070 mL | |
| 100 mM | 0.0130 mL | 0.0651 mL | 0.1302 mL | 0.3256 mL |