Acetaminophen-Paracetamol-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAcetaminophenCat. No.: HY-66005CAS No.: 103-90-2Synonyms: Paracetamol; 4-Hydroxyacetanilide; 4-Acetamidophenol;APAP分式: CHNO分量: 151.16作靶点: COX; Endogenous Metabolite作通路: Immunology/Inflammation; Metabolic Enzyme/Protease储存式: Powd

2、er -20C 3 years4C 2 years* 该产品在溶液状态不稳定，建议您现现配，即刻使。溶解性数据体外实验 DMSO : 100 mg/mL (661.55 mM)H2O : 10 mg/mL (66.16 mM; Need ultrasonic)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 6.6155 mL 33.0775 mL 66.1551 mL5 mM 1.3231 mL 6.6155 mL 13.2310 mL10 mM 0.6616

3、mL 3.3078 mL 6.6155 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液；该产品在溶液状态不稳定，建议您现现配，即刻使。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (16.54 mM); Clear solut

4、ion1/3 Master of Small Molecules 您边的抑制剂师www.MedChemE2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (16.54 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (16.54 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Acetaminophen (paracetamol)选择性环氧合酶-2 (COX-2)

5、的抑制剂，IC50 值为 25.8 M。它 泛使的解热和痛药。IC50 & Target COX-2 COX-1 Human Endogenous Metabolite25.8 M (IC50) 113.7 M (IC50)体外研究 In vitro, acetaminophen elicites a 4.4-fold selectivity toward COX-2 inhibition (IC50 113.7 M for COX-1; IC5025.8 M for COX-2). Following oral administration of the drug, maximal ex v

6、ivo inhibitions are 56% (COX-1)and 83% (COX-2). Acetaminophen plasma concentrations remaine above the in vitro IC50 for COX-2 for atleast 5 h postadministration. Ex vivo IC50 values (COX-1: 105.2 M; COX-2: 26.3 M) of acetaminophencompared favorably with its in vitro IC50 values. In contrast to previ

7、ous concepts, acetaminophen inhibitedCOX-2 by more than 80%, i.e., to a degree comparable to nonsteroidal antiinflammatory drugs (NSAIDs) andselective COX-2 inhibitors. However, a 95% COX-1 blockade relevant for suppression of platelet function isnot achieved 1. MTT assay shows that Acetaminophen (A

8、PAP) in a dose of 50 mM significantly (p 2.体内研究 Administering Acetaminophen (250mg/kg, orally) to the mice causes significant (p 3.PROTOCOLCell Assay 2 Human hepatoma cell line HepG2 is cultured in low glucose DMEM supplemented with 10% fetal bovineserum (FBS), 100 U/mL Penicillin and 100 g/mL Strep

9、tomycin and 2 mM l-glutamine. The cells aremaintained in 75 cm2 flasks at 37C in a humidified atmosphere containing 5% CO2 and split at 80%confluence every 5 days. Cells are seeded in 24-well plate (2105 cells) and incubated at 37C overnightfollowed by cells pretreatment with complete DMEM containin

10、g high glucose concentration in order todownregulate autophagy. After 6 h, cells are treated with different concentrations of postbiotics obtained fromLactobacillus fermentum BGHV110 strain (HV110) in order to select appropriate dose for furtherexperiments. Postbiotic is dissolved in complete DMEM m

11、edium and added to the cells in specific finalconcentration. 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

12、 lysosomotropic agent Chloroquine at a concentration of25 M, to inhibit autophagosome-lysosome fusion 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 3Administration 3 Male Swiss mice (30-40g) are used. The experimental animals are divided

13、 into six groups of five animals2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEeach. Firstly, each group receive orally during seven days the following treatment: Group I: the mice do notreceive any treatment (normal). Group II: the mice receive citral vehicle (0.1% Tween 80 solution). Groups III-

14、V: the mice are pretreated with citral at doses of 125, 250, and 500mg/kg, respectively. Group VI: the miceare pretreated with the hepatoprotective standard drug Silymarin (SLM) (200mg/kg). After this time, theanimals fasted for 8h and then receive oral Acetaminophen on the seventh day at a dose of

15、250mg/kg inGroups 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 50mg/mL and after that is diluted in 0.1% Tween 80solution to prepare the solutions of 25 and 12.5mg/mL. After 12h of Acetamin

16、ophen administration, serumsamples 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.户使本产品发表的科研献 Theranostics. 2017 Sep 26;7(17):4135-4148. Lab Chip. 2018 Nov 6;18(22):3379-

17、3392. Chemosphere. 2019 Mar. Front Pharmacol. 2017 Sep 19;8:653. Appl Microbiol Biotechnol. 2018 Feb;102(3):1443-1453.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Hinz, B, et al. Acetaminophen (paracetamol) is a selective cyclooxygenase-2 inhibitor in man. FASEB J, 2008. 22(2): p. 383-90.2. Dini? M, et al. Lactobacillus fermentum Postbiotic-induced Autophagy as Potential Approach for Treatment ofAcetaminophenHepatotoxicity. Front Microbiol. 2017 Apr 6;8:594.3. Uchida NS, et al. Hepatoprotective Effect of Citral on Acetaminophen-Induced Liver T