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  4. Propacetamol

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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Propacetamol

Propacetamol Chemical Structure

CAS No. : 66532-85-2

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Based on 1 publication(s) in Google Scholar

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Propacetamol Related Antibodies

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Description

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[1][2][3].

In Vivo

Propacetamol (1200 mg/kg, i.p., single dose) induces acute liver injury in BALB/c mice[1].
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.

Animal Model: Five-week-old male BALB/c mice[1]
Dosage: 1200 mg/kg
Administration: i.p., single dose
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.
Animal Model: Male Kunming mice (25-30 g) injected with Acetic acid[2]
Dosage: 200 mg/kg
Administration: i.p., once, 15 min before acetic acid injection
Result: Exerted significant antinociceptive effect in male Kunming mice by reducing the number of writhes.
Animal Model: Male Wistar rats injected with ASA[3]
Dosage: 125, 250, 500 mg/kg
Administration: i.g., once, 30 min before ASA administration
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.
Clinical Trial
Molecular Weight

264.32

Formula

C14H20N2O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(OC1=CC=C(NC(C)=O)C=C1)CN(CC)CC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.7833 mL 18.9165 mL 37.8329 mL
5 mM 0.7567 mL 3.7833 mL 7.5666 mL
View the 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.

* 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.

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  • Dilution Calculator

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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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (9.46 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

  • Protocol 2

    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.

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.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 100 mg/mL (378.33 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
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. 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.

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Propacetamol66532-85-2Interleukin RelatedILanalgesicprecursorparacetamolpostoperative painacute traumagastrointestinal disordersInhibitorinhibitorinhibit

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