1. Immunology/Inflammation
    Epigenetics
    Metabolic Enzyme/Protease
  2. COX
    Histone Acetyltransferase
    Endogenous Metabolite
  3. Acetaminophen

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

Cat. No.: HY-66005 Purity: 99.69%
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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 drug. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor.

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Acetaminophen Chemical Structure

Acetaminophen Chemical Structure

CAS No. : 103-90-2

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Customer Review

Based on 13 publication(s) in Google Scholar

Top Publications Citing Use of Products

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

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

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

    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 MCE. Usage Cited in: Molecules. 2018 Dec 29;24(1). pii: E110.

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

    Acetaminophen purchased from MCE. Usage Cited in: Molecules. 2018 Dec 29;24(1). pii: E110.

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

    Acetaminophen purchased from MCE. Usage Cited in: Molecules. 2018 Dec 29;24(1). pii: E110.

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

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    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 drug[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)

    Human Endogenous Metabolite

     

    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].

    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].

    Clinical Trial
    Molecular Weight

    151.16

    Formula

    C₈H₉NO₂

    CAS No.

    103-90-2

    SMILES

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

    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 : ≥ 100 mg/mL (661.55 mM)

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

    *"≥" means soluble, but saturation unknown.

    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
    10 mM 0.6616 mL 3.3078 mL 6.6155 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (16.54 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (16.54 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (16.54 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    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
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    Keywords:

    AcetaminophenParacetamol4'-Hydroxyacetanilide4-AcetamidophenolAPAPCOXHistone AcetyltransferaseEndogenous MetaboliteCyclooxygenaseHATsHATInhibitorinhibitorinhibit

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