Propacetamol
Based on 1 Customer Validation
Propacetamol is an orally active prodrug of Acetaminophen (HY-66005), which exerts antipyretic and analgesic effects after metabolism. Propacetamol reduces Aspirin (ASA) (HY-14654)-induced elevation of malondialdehyde (MDA) in gastric mucosa and plasma, regulates the levels of gastric mucosal glutathione (GSH and GSSG) to maintain cellular antioxidant defense, and increases gastric mucosal uric acid (UA) levels. Propacetamol exerts a dose-dependent protective effect against ASA-induced gastric mucosal damage in rats. Propacetamol can be used for the study of gastric mucosal injury by interfering with oxidative stress.
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- Pureza: 98.02%
- No. CAS: 66532-85-2
- Fòrmula: C14H20N2O3
- Peso molecular:264.32
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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
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Actividad biológica
Propacetamol (200 mg/kg, i.p., once, 15 min before Acetic acid (HY-Y0319) injection) exerts significant antinociceptive effect in male Kunming mice[2].
Propacetamol (125-500 mg/kg, i.g., once) exerts a dose-dependent gastroprotective effect in male Wistar rats with Aspirin (acetylsalicylic acid; ASA) (HY-14654)-induced gastric mucosal damage[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Five-week-old male BALB/c mice[1]
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Dosage:1200 mg/kg
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Administration:i.p., single dose
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Result:Creased serum ALT/AST activities, hepatic pericentral necrosis.
Exhausted hepatic GSH levels.
Elevated MDA and 3-NT levels.
Decreased SOD and GPx activities.
Increased serum/hepatic TNF-α and IL-6 levels.
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Animal Model:Male Kunming mice (25-30 g) injected with Acetic acid[2]
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Dosage:200 mg/kg
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Administration:i.p., once, 15 min before acetic acid injection
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Result:Exerted significant antinociceptive effect in male Kunming mice by reducing the number of writhes.
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Animal Model:Male Wistar rats injected with ASA[3]
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Dosage:125, 250, 500 mg/kg
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Administration:i.g., once, 30 min before ASA administration
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Result:Reduced the ulcer area.
Decreased the elevated gastric mucosal MDA level.
Increased the reduced gastric mucosal UA level.
Reduced the elevated gastric mucosal GSH and GSSG levels.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 66532-85-2
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Appearance Solid
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Peso molecular 264.32
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Fòrmula C14H20N2O3
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Color White to off-white
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SMILES
O=C(OC1=CC=C(NC(C)=O)C=C1)CN(CC)CC
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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
H2O : 100 mg/mL (378.33 mM; Need ultrasonic)
DMSO : 33.33 mg/mL (126.10 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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (7.87 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 (7.87 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 100 mg/mL (378.33 mM); Clear solution; Need ultrasonic
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Pureza y Documentación
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Ficha de datos (275 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
[1]. Liou GG, et al. N-Acetyl Cysteine Overdose Inducing Hepatic Steatosis and Systemic Inflammation in Both Propacetamol-Induced Hepatotoxic and Normal Mice. Antioxidants (Basel). 2021 Mar 12;10(3):442. [Content Brief]
[2]. Zhang Y, et al. Enhanced analgesic effects of propacetamol and tramadol combination in rats and mice. Biol Pharm Bull. 2011;34(3):349-53. doi: 10.1248/bpb.34.349 [Content Brief]
[3]. Galunska B, et al. Effects of paracetamol and propacetamol on gastric mucosal damage and gastric lipid peroxidation caused by acetylsalicylic acid (ASA) in rats. Pharmacol Res. 2002 Aug;46(2):141-7. [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 / H2O | 1 mM | 3.7833 mL | 18.9165 mL | 37.8329 mL | 94.5823 mL |
| 5 mM | 0.7567 mL | 3.7833 mL | 7.5666 mL | 18.9165 mL | |
| 10 mM | 0.3783 mL | 1.8916 mL | 3.7833 mL | 9.4582 mL | |
| 15 mM | 0.2522 mL | 1.2611 mL | 2.5222 mL | 6.3055 mL | |
| 20 mM | 0.1892 mL | 0.9458 mL | 1.8916 mL | 4.7291 mL | |
| 25 mM | 0.1513 mL | 0.7567 mL | 1.5133 mL | 3.7833 mL | |
| 30 mM | 0.1261 mL | 0.6305 mL | 1.2611 mL | 3.1527 mL | |
| 40 mM | 0.0946 mL | 0.4729 mL | 0.9458 mL | 2.3646 mL | |
| 50 mM | 0.0757 mL | 0.3783 mL | 0.7567 mL | 1.8916 mL | |
| 60 mM | 0.0631 mL | 0.3153 mL | 0.6305 mL | 1.5764 mL | |
| 80 mM | 0.0473 mL | 0.2365 mL | 0.4729 mL | 1.1823 mL | |
| 100 mM | 0.0378 mL | 0.1892 mL | 0.3783 mL | 0.9458 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Propacetamol Related Classifications
HY-145453 Related Classifications
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