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Acetaminophen  (Synonyms: Paracetamol; 4-Acetamidophenol; 4'-Hydroxyacetanilide)

Cat. No.: HY-66005 Purity: 99.98%
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Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM; is a widely used antipyretic and analgesic agent. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor.

For research use only. We do not sell to patients.

Acetaminophen Chemical Structure

Acetaminophen Chemical Structure

CAS No. : 103-90-2

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Customer Review

Based on 38 publication(s) in Google Scholar

Other Forms of Acetaminophen:

Top Publications Citing Use of Products

33 Publications Citing Use of MCE Acetaminophen

WB

    Acetaminophen purchased from MedChemExpress. Usage Cited in: Appl Microbiol Biotechnol. 2018 Feb;102(3):1443-1453.  [Abstract]

    Dihydroquercetin relieves APAP-induced necrosis and suppressed ERK/JNK stress responses. Western Blot analysis for phosphor-JNK1/2, β-Actin as a lading control.

    Acetaminophen purchased from MedChemExpress. Usage Cited in: Molecules. 2018 Dec 29;24(1). pii: E110.  [Abstract]

    Western analysis of p-Akt protein expression with or without the treatment of APAP.

    Acetaminophen purchased from MedChemExpress. Usage Cited in: Molecules. 2018 Dec 29;24(1). pii: E110.  [Abstract]

    Western analysis of p-Akt protein expression in L-02 cells with or without the treatment of APAP and SHK.

    Acetaminophen purchased from MedChemExpress. Usage Cited in: Molecules. 2018 Dec 29;24(1). pii: E110.  [Abstract]

    Western analysis of Nrf2 protein expression in L-02 cells with or without the treatment of APAP and SHK.

    Acetaminophen purchased from MedChemExpress. Usage Cited in: Theranostics. 2017 Sep 26;7(17):4135-4148.  [Abstract]

    LiposIA inhibits ROS generation and prevents APAP-induced mitochondrial dysfunction in the liver. Immunoblot images of iNOS and p-JNK.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM; is a widely used antipyretic and analgesic agent[1][2][3]. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor[4].

    IC50 & Target[1]

    COX-2

    25.8 μM (IC50)

    COX-1

    113.7 μM (IC50)

    In Vitro

    In vitro, acetaminophen elicites a 4.4-fold selectivity toward COX-2 inhibition (IC50 113.7 μM for COX-1; IC50 25.8 μM for COX-2). Following oral administration of the drug, maximal ex vivo inhibitions are 56% (COX-1) and 83% (COX-2). Acetaminophen plasma concentrations remaine above the in vitro IC50 for COX-2 for at least 5 h postadministration. Ex vivo IC50 values (COX-1: 105.2 μM; COX-2: 26.3 μM) of acetaminophen compared favorably with its in vitro IC50 values. In contrast to previous concepts, acetaminophen inhibited COX-2 by more than 80%, i.e., to a degree comparable to nonsteroidal antiinflammatory drugs (NSAIDs) and selective COX-2 inhibitors. However, a >95% COX-1 blockade relevant for suppression of platelet function is not achieved[1]. MTT assay shows that Acetaminophen (APAP) in a dose of 50 mM significantly (p<0.001) reduces cell viability to 61.5±6.65%. Interestingly, the significant (p<0.01) increase in cell viability to 79.7±2.47% is observed in the Acetaminophen/HV110 co-treated cells, compared to Acetaminophen treated cells[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    In Vivo

    Administering Acetaminophen (250 mg/kg, orally) to the mice causes significant (p<0.001) liver damage and necrosis of cells as evidenced by the elevated serum hepatic enzymes alanine aminotransferase (ALT), aminotransferase (AST), alkaline phosphatase (ALP), and gamma-glutamyl transferase (γGT) compared with normal group. Conversely, effects of pretreatment with different doses of citral (125, 250, and 500 mg/kg) exhibited a significant (p<0.05) decrease in serum activities of ALT (91.79%, 93.07%, and 95.61%, resp.), AST (93.40%, 91.89%, and 96.52%, resp.), ALP (39.29%, 37.07%, and 59.80%, resp.), and γGT (92.83%, 91.59%, and 93.0%, resp.), when compared to the Acetaminophen group. Similar results were found in pretreatment with SLM on the activity of ALT (95.90%), AST (95.03%), ALP (70.52%), and γGT (92.69%)[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    Molecular Weight

    151.16

    Formula

    C8H9NO2

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C)NC1=CC=C(O)C=C1

    Structure Classification
    Initial Source
    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years

    *The compound is unstable in solutions, freshly prepared is recommended.

    Solvent & Solubility
    In Vitro: 

    DMSO : 250 mg/mL (1653.88 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 10 mg/mL (66.16 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 6.6155 mL 33.0775 mL 66.1551 mL
    5 mM 1.3231 mL 6.6155 mL 13.2310 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

    * 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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    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: 6.67 mg/mL (44.13 mM); Clear solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  50% PEG300    50% Saline

      Solubility: 66.67 mg/mL (441.06 mM); Clear solution; Need ultrasonic and heat to 30°C

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

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    Purity & Documentation

    Purity: 99.98%

    References
    Cell Assay
    [2]

    Human hepatoma cell line HepG2 is cultured in low glucose DMEM supplemented with 10% fetal bovine serum (FBS), 100 U/mL Penicillin and 100 μg/mL Streptomycin and 2 mM l-glutamine. The cells are maintained in 75 cm2 flasks at 37°C in a humidified atmosphere containing 5% CO2 and split at 80% confluence every 5 days. Cells are seeded in 24-well plate (2×105 cells) and incubated at 37°C overnight followed by cells pretreatment with complete DMEM containing high glucose concentration in order to downregulate autophagy. After 6 h, cells are treated with different concentrations of postbiotics obtained from Lactobacillus fermentum BGHV110 strain (HV110) in order to select appropriate dose for further experiments. Postbiotic is dissolved in complete DMEM medium and added to the cells in specific final concentration. In all other experiments seeded cells are treated with 50 mM Acetaminophen alone or co-treated with 50 mM Acetaminophen and selected dose of lyophilized HV110. To analyze autophagic flux, simultaneously with treatments, cells are exposed to lysosomotropic agent Chloroquine at a concentration of 25 μM, to inhibit autophagosome-lysosome fusion[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3]

    Mice[3]
    Male Swiss mice (30-40 g) are used. The experimental animals are divided into six groups of five animals each. Firstly, each group receive orally during seven days the following treatment: Group I: the mice do not receive any treatment (normal). Group II: the mice receive citral vehicle (0.1% Tween 80 solution). Groups III-V: the mice are pretreated with citral at doses of 125, 250, and 500 mg/kg, respectively. Group VI: the mice are pretreated with the hepatoprotective standard drug Silymarin (SLM) (200 mg/kg). After this time, the animals fasted for 8 h and then receive oral Acetaminophen on the seventh day at a dose of 250 mg/kg in Groups II-VI. Group I orally receive saline that contained 0.1% Tween 80 solution (Acetaminophen vehicle). The stock solution is used as the first concentration of 50 mg/mL and after that is diluted in 0.1% Tween 80 solution to prepare the solutions of 25 and 12.5 mg/mL. After 12 h of Acetaminophen administration, serum samples and liver tissue are collected followed by biochemistry and histological analysis.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 6.6155 mL 33.0775 mL 66.1551 mL 165.3877 mL
    5 mM 1.3231 mL 6.6155 mL 13.2310 mL 33.0775 mL
    10 mM 0.6616 mL 3.3078 mL 6.6155 mL 16.5388 mL
    15 mM 0.4410 mL 2.2052 mL 4.4103 mL 11.0258 mL
    20 mM 0.3308 mL 1.6539 mL 3.3078 mL 8.2694 mL
    25 mM 0.2646 mL 1.3231 mL 2.6462 mL 6.6155 mL
    30 mM 0.2205 mL 1.1026 mL 2.2052 mL 5.5129 mL
    40 mM 0.1654 mL 0.8269 mL 1.6539 mL 4.1347 mL
    50 mM 0.1323 mL 0.6616 mL 1.3231 mL 3.3078 mL
    60 mM 0.1103 mL 0.5513 mL 1.1026 mL 2.7565 mL
    DMSO 80 mM 0.0827 mL 0.4135 mL 0.8269 mL 2.0673 mL
    100 mM 0.0662 mL 0.3308 mL 0.6616 mL 1.6539 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.

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