Acetaminophen

Catalog No.S1634 Batch:S163404

Technical Data

Formula

C₈H₉NO₂

Molecular Weight

151.16

CAS No.

103-90-2

Solubility (25°C)*

In vitro

DMSO

600 mg/mL (3969.3 mM)

Ethanol

30 mg/mL (198.46 mM)

Water

5 mg/mL (33.07 mM)

In vivo (Add solvents to the product individually and in order)

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	30.000mg/ml (198.47mM)	Taking the 1 mL working solution as an example, add 50 μL of 600 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

Acetaminophen is a COX inhibitor for COX-1 and COX-2 with IC50 of 113.7 μM and 25.8 μM, respectively.

Targets

COX2 ^[1]	COX1 ^[1]
25.8 μM	113.57 μM

In vitro

Acetaminophen is functionally active as a selective COX-2 inhibitor, exhibiting a 4.4-fold specificity towards COX-2 (IC50 is 113.7 μM for COX-1 and IC50 of 25.8 μM for COX-2). This compound demonstrates selective toxicity towards melanoma cells, such as SK-MEL-28, MeWo, SK-MEL-5, B16-F0 and B16-F10, with IC50 of 100 μM, and shows no significant toxicity towards BJ, Saos-2, SW-620, and PC-3 non-melanoma cells. It induces the apoptosis of SK-MEL-28 cells through intracellular GSH depletion, ROS formation and induced mitochondrial toxicity, which can be enhanced by Dicoumarol and 1-bromoheptane and allayed by Ascorbic acid, GSH, Trifluoperazine and cyclosporin A. This chemical significantly inhibits the activity of COX-2 which has been induced by diclofenac than that induced by bacterial lipopolysaccharide in murine J774.2 macrophages. However in the presence of diclofenac, LPS-induced COX-2 activity is inhibited by it to the same extent as the COX-2 activity induced by diclofenac alone.

In vivo

Overdose of Acetaminophen leads to liver toxicity, which is well correlated with liver protein arylation by its metabolites. Administration of this compound (1 g/kg) in male Long Evans Hooded rats causes damage to centrilobular regions of the liver, increases serum transaminase levels significantly within 6 hours of treatment, reaching a maximum at 24 hours. This can be correlated to expression of the inducible nitric oxide synthase (iNOS) protein.

Features

Acetaminophen has analgesic properties comparable to those of aspirin, while its anti-inflammatory effects are weaker.

Protocol (from reference)

Kinase Assay:^{^[1]}	Effect of inhibition of Acetaminophen on COX-1 and COX-2 activity in human whole blood For COX-1 assay, aliquots of human whole blood drawn from healthy volunteers without anticoagulant are transferred to glass tubes containing Acetaminophen or DMSO, serum is separated by centrifugation after clotting, and serum TxB2 levels are determined. For COX-2 assay, aliquots of heparinized whole blood are incubated with LPS (10 μg/mL) and aspirin (10 μg/mL), plus this compound or DMSO for 24 hours at 37 °C, plasma is separated by centrifugation, and PGE2 levels are determined subsequently. The degree of COX-1 or COX-2 inhibition is calculated as the percentage change of plasma eicosanoid (TxB2 for COX-1 and PGE2 for COX-2).Concentration response curves are fitted by a sigmoidal regression with variable slope for both enzymatic assays, and the 50% inhibitory concentration (IC50) values are derived by using of PRISM Version 3.0.
Cell Assay:^{^[2]}	Cell lines SK-MEL-28, SK-MEL-5, MeWo, Saos-2, SW-620, PC-3, B16-F0, B16-F10, BJ fibroblast cell lines and Human epidermal melanocytes Concentrations Dissolved in DMSO, final concentration ~500 μM Incubation Time 48 hours Method Cells are exposed to Acetaminophen for 48 hours. Cell viability is determined by the trypan blue exclusion method. Intracellular GSH is measured by recording the disulfide, GS-TNB and 5-thio-nitrobenzoic acid (TNB), the yellow colored compound formed by the reaction between GSH with DTNB.
Animal Study:^{^[4]}	Animal Models B6C3F1 mice Dosages 350 mg/kg Administration Oral daily

References

https://pubmed.ncbi.nlm.nih.gov/17884974/
https://pubmed.ncbi.nlm.nih.gov/18759348/
https://pubmed.ncbi.nlm.nih.gov/10077674/

https://pubmed.ncbi.nlm.nih.gov/9651401/
https://pubmed.ncbi.nlm.nih.gov/9500703/

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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