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Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM. Acetaminophen is a widely used antipyretic and analgesic agent. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor. Acetaminophen induces ferroptosis and leads to acute liver injury in mice model.
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.
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. Acetaminophen (300 mg/kg, i.p., single dose) induces ferroptosis, by enhancing levels of Fe2+ and malondialdehyde (MDA), and decreasing levels of glutathione (GSH) and glutathione peroxidase 4 (GPX4), and induces acut eliver injury in C57BL/6J mice model.
*The compound is unstable in solutions, freshly prepared is recommended
FASEB J. 2025 Jan 07;39(1):e70272.
The C3/C3aR pathway exacerbates acetaminophen‐induced mouse liver injury via upregulating podoplanin on the macrophage
Acetaminophen purchased from AbMole
| Molecular Weight | 151.16 |
| Formula | C8H9NO2 |
| CAS Number | 103-90-2 |
| Solubility (25°C) | DMSO 60 mg/mL Water 10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Clyde J Wright. Acetaminophen and the Developing Lung: Could There Be Lifelong Consequences?
[3] Anita Aminoshariae, et al. Acetaminophen: old drug, new issues
[4] K Brune, et al. Acetaminophen/paracetamol: A history of errors, failures and false decisions
[5] Marta Jźwiak-Bebenista, et al. Paracetamol: mechanism of action, applications and safety concern
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