AEP-IN-3
Based on 1 Customer Validation
AEP-IN-3 (compound 18) is an orally active, potent and brain penetrant asparagine endopeptidase (AEP) inhibitor, with an IC50 of 7.8 ± 0.9 nM. AEP-IN-3 can be used for Alzheimer’s Disease (AD) research.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.95%
- No. CAS: 2978521-26-3
- Fòrmula: C21H21F4N3O4
- Peso molecular:455.40
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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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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
Descripciòn
In Vivo
AEP-IN-3 (20 mg/kg, orally, BID, for 5 days) shows significantly inhibited activity of AEP in brain in TauP301L transgenic mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice producing the 2N4R isoform of human Tau containing the P301L mutation in a FVB/N genetic background (3.8 months old)[1]
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Dosage:20 mg/kg
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Administration:Orally, BID with an interval of 7-8 h between doses for 5 days
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Result:Showed significantly inhibited activity of AEP in brain, reduced formation of the Tau N368 fragment. The effect on total Tau is not significant.
Chemical Information
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No. CAS 2978521-26-3
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Appearance Solid
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Peso molecular 455.40
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Fòrmula C21H21F4N3O4
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Color White to off-white
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SMILES
O=C(N1C[C@H](F)C[C@H]1C(N[C@@H](CC(N)=O)C#C)=O)C2(CC2)C3=CC=C(OC(F)(F)F)C=C3
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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
In Vitro:
DMSO : 100 mg/mL (219.59 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)
In Vivo:
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: 2.5 mg/mL (5.49 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.49 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
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 (280 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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. 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 | 2.1959 mL | 10.9794 mL | 21.9587 mL | 54.8968 mL |
| 5 mM | 0.4392 mL | 2.1959 mL | 4.3917 mL | 10.9794 mL | |
| 10 mM | 0.2196 mL | 1.0979 mL | 2.1959 mL | 5.4897 mL | |
| 15 mM | 0.1464 mL | 0.7320 mL | 1.4639 mL | 3.6598 mL | |
| 20 mM | 0.1098 mL | 0.5490 mL | 1.0979 mL | 2.7448 mL | |
| 25 mM | 0.0878 mL | 0.4392 mL | 0.8783 mL | 2.1959 mL | |
| 30 mM | 0.0732 mL | 0.3660 mL | 0.7320 mL | 1.8299 mL | |
| 40 mM | 0.0549 mL | 0.2745 mL | 0.5490 mL | 1.3724 mL | |
| 50 mM | 0.0439 mL | 0.2196 mL | 0.4392 mL | 1.0979 mL | |
| 60 mM | 0.0366 mL | 0.1830 mL | 0.3660 mL | 0.9149 mL | |
| 80 mM | 0.0274 mL | 0.1372 mL | 0.2745 mL | 0.6862 mL | |
| 100 mM | 0.0220 mL | 0.1098 mL | 0.2196 mL | 0.5490 mL |
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