Aleplasinin
Based on 1 Customer Validation
Aleplastinin (PAZ-417) is an orally active, blood-brain barrier permeable, selective SERPINE1 (PAI-1) inhibitor (IC50=655 nM). Aleplastinin activates the tissue type plasminogen activator (tPA)/fibrinolysis cascade by inhibiting PAI-1, thereby promoting the degradation of amyloid-β (Aβ) oligomers and monomers. Aleplastinin can significantly reduce plasma and brain Aβ levels, improve memory impairment, and reverse cognitive impairment. Aleplastinin can be used for research on Alzheimer's disease.
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- Pureza: 99.59%
- No. CAS: 481629-87-2
- Fòrmula: C28H27NO3
- Peso molecular:425.52
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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
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PAI-1 655 nM (IC50) |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Tg2576 transgenic mice (male, 20-week-old, expressing human APPSwedish mutation), Alzheimer's disease model[1]
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Dosage:20 mg/kg
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Administration:Oral gavage, single dose, 6 h prior to euthanasia.
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Result:Decreased plasma Aβ40 by 26% (p<0.001), brain Aβ40 and reduced Aβ42 by 22% and 21%, respectively.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 481629-87-2
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Appearance Solid
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Peso molecular 425.52
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Fòrmula C28H27NO3
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Color Off-white to light yellow
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SMILES
O=C(O)C(C1=CN(CC2=CC=C(C(C)(C)C)C=C2)C3=C1C=C(C4=CC=CC(C)=C4)C=C3)=O
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Synonyms
PAZ-417
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvente y solubilidad
DMSO : 250 mg/mL (587.52 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)
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: ≥ 2.08 mg/mL (4.89 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.89 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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 (protect from 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.
Pureza y Documentación
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Ficha de datos (276 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]. Jacobsen JS, et al. Enhanced clearance of Abeta in brain by sustaining the plasmin proteolysis cascade. Proc Natl Acad Sci U S A. 2008 Jun 24;105(25):8754-9. [Content Brief]
[2]. Kellici TF, et al. Therapeutic Potential of Targeting Plasminogen Activator Inhibitor-1 in COVID-19. Trends Pharmacol Sci. 2021 Jun;42(6):431-433. [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 (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 | 2.3501 mL | 11.7503 mL | 23.5007 mL | 58.7516 mL |
| 5 mM | 0.4700 mL | 2.3501 mL | 4.7001 mL | 11.7503 mL | |
| 10 mM | 0.2350 mL | 1.1750 mL | 2.3501 mL | 5.8752 mL | |
| 15 mM | 0.1567 mL | 0.7834 mL | 1.5667 mL | 3.9168 mL | |
| 20 mM | 0.1175 mL | 0.5875 mL | 1.1750 mL | 2.9376 mL | |
| 25 mM | 0.0940 mL | 0.4700 mL | 0.9400 mL | 2.3501 mL | |
| 30 mM | 0.0783 mL | 0.3917 mL | 0.7834 mL | 1.9584 mL | |
| 40 mM | 0.0588 mL | 0.2938 mL | 0.5875 mL | 1.4688 mL | |
| 50 mM | 0.0470 mL | 0.2350 mL | 0.4700 mL | 1.1750 mL | |
| 60 mM | 0.0392 mL | 0.1958 mL | 0.3917 mL | 0.9792 mL | |
| 80 mM | 0.0294 mL | 0.1469 mL | 0.2938 mL | 0.7344 mL | |
| 100 mM | 0.0235 mL | 0.1175 mL | 0.2350 mL | 0.5875 mL |
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