Acetaminophen

製品コードS1634 バッチS163404

印刷

化学情報

Synonyms

Paracetamol, Tylenol, APAP

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₈H₉NO₂

分子量

151.16

CAS No.

103-90-2

Solubility (25°C)*

体外

DMSO

600 mg/mL (3969.3 mM)

Ethanol

30 mg/mL (198.46 mM)

Water

5 mg/mL (33.07 mM)

体内（毎回新しく調製した物を用意してください）

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 この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Acetaminophenは、COX-1およびCOX-2のCOX阻害剤であり、それぞれのIC50は113.7 μMおよび25.8 μMです。
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.
特徴	Acetaminophen has analgesic properties comparable to those of aspirin, while its anti-inflammatory effects are weaker.

プロトコル(参考用のみ)

キナーゼアッセイ	Effect of inhibition of Acetaminophen on COX-1 and COX-2 activity in human whole blood
キナーゼアッセイ	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.
細胞アッセイ	細胞株	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
	濃度	Dissolved in DMSO, final concentration ~500 μM
	反応時間	48 hours
	実験の流れ	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.
動物実験	動物モデル	B6C3F1 mice
	投薬量	350 mg/kg
	投与方法	Oral daily

参考

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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長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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