QC-01–175
Based on 1 Customer Validation
QC-01-175 is a Tau PROTAC degrader, with Kd values of 1.2 μM, 1.7 μM and 2.5 μM for wild-type, A152T mutant and P301L mutant tau-441 proteins, respectively. QC-01-175 binds to both Tau and CRBN, triggering ubiquitination and proteasomal degradation of Tau. QC-01-175 preferentially targets disease-associated Tau proteins in frontotemporal dementia. QC-01-175 inhibits MAO activity, with an IC50 of 8.56 μM. QC-01-175 suppresses the elevation of ROS levels. QC-01-175 can be used in studies related to frontotemporal dementia and amyotrophic lateral sclerosis.
(Pink: Tau Protein ligand (HY-W453397); Blue: Cereblon ligand (HY-10984); Black: linker (HY-W007545)).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.94%
- No. CAS: 2267290-96-8
- Fòrmula: C33H34N6O7
- Peso molecular:626.66
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Chemical Information
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Solvente y solubilidad
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Actividad biológica
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Cereblon |
QC-01-175 binds to recombinant wild-type, A152T mutant, and P301L mutant tau-441 proteins respectively, with corresponding KD values of 1.2 μM, 1.7 μM, and 2.50 μM[1].
QC-01-175 (10 μM; 4 h) significantly reduces the level of pTau-S396 in SH-SY5Y cells treated with ALS SNs[2].
QC-01-175 (60 min) inhibits MAO activity with an IC50 of 8.56 μM, and its off-target MAO inhibitory effect is reduced compared with the parent compound T807[1].
QC-01-175 (10 μM; 4 h) prevents the increase in reactive oxygen species levels in SH-SY5Y cells induced by tau protein and ALS sensory neurons (SNs)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:6-week differentiated FTD patient-derived A152T iPSC cortical neurons
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Concentration:10 μM
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Incubation Time:Not specified
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Result:Reduced total tau and P-tau S396/S404 immunofluorescence signal relative to vehicle or inactive analog QC-03-075-treated neurons.
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Cell Line:human neuroblastoma SH-SY5Y cells
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Concentration:1 μM, 10 μM
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Incubation Time:2 h, 4 h, 24 h
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Result:Showed no effect on pTau-S396 levels in ALS SNs-treated cells across all time points at 1 μM.
Reduced pTau-S396 levels in ALS SNs-treated cells after 4 h, with the effect absent after 24 h at 10 μM.
Caused a significant decrease in pTau-S396 levels in ALS SNs+QC-01-175-treated cells compared to ALS SNs-only treated cells (one-way ANOVA, F(3,12) = 3.699, p = 0.0429; Tukey’s test, p = 0.0328) in a confirmatory assay at 10 μM for 4 h.
Chemical Information
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No. CAS 2267290-96-8
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Appearance Solid
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Peso molecular 626.66
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Fòrmula C33H34N6O7
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Color Light yellow to green yellow
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SMILES
O=C(NCCOCCOCCNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CCC4=CC5=C(C=C4)C(C=NC=C6)=C6N5
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (159.58 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)
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: ≥ 5 mg/mL (7.98 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
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.
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Silva MC, et al. Targeted degradation of aberrant tau in frontotemporal dementia patient-derived neuronal cell models. eLife. 2019 Mar 25;8:e45457. [Content Brief]
[2]. Petrozziello T, et al. Targeting Tau Mitigates Mitochondrial Fragmentation and Oxidative Stress in Amyotrophic Lateral Sclerosis. Molecular neurobiology. 2022 Jan;59(1):683-702. [Content Brief]
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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.5958 mL | 7.9788 mL | 15.9576 mL | 39.8940 mL |
| 5 mM | 0.3192 mL | 1.5958 mL | 3.1915 mL | 7.9788 mL | |
| 10 mM | 0.1596 mL | 0.7979 mL | 1.5958 mL | 3.9894 mL | |
| 15 mM | 0.1064 mL | 0.5319 mL | 1.0638 mL | 2.6596 mL | |
| 20 mM | 0.0798 mL | 0.3989 mL | 0.7979 mL | 1.9947 mL | |
| 25 mM | 0.0638 mL | 0.3192 mL | 0.6383 mL | 1.5958 mL | |
| 30 mM | 0.0532 mL | 0.2660 mL | 0.5319 mL | 1.3298 mL | |
| 40 mM | 0.0399 mL | 0.1995 mL | 0.3989 mL | 0.9974 mL | |
| 50 mM | 0.0319 mL | 0.1596 mL | 0.3192 mL | 0.7979 mL | |
| 60 mM | 0.0266 mL | 0.1330 mL | 0.2660 mL | 0.6649 mL | |
| 80 mM | 0.0199 mL | 0.0997 mL | 0.1995 mL | 0.4987 mL | |
| 100 mM | 0.0160 mL | 0.0798 mL | 0.1596 mL | 0.3989 mL |
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