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Acetaminophen

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Chemical Structure| 103-90-2 同义名 : 对乙酰氨基酚;N-(4-羟基苯基)乙酰胺;对乙酰氨基苯酚;醋氨酚 ;Paracetamol;4-Acetamidophenol;NSC 109028;NSC 3991;Acetaminophen (CRM);APAP;Tylenol;4'-Hydroxyacetanilide
CAS号 : 103-90-2
货号 : A660637
分子式 : C8H9NO2
纯度 : 98%
分子量 : 151.16
MDL号 : MFCD00002328
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL(1653.85 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 10 mg/mL(66.15 mM)，配合低频超声助溶
动物实验配方：
生物活性
描述 Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM; is a widely used antipyretic and analgesic agent. In vitro, acetaminophen elicited a 4.4-fold selectivity toward COX-2 inhibition (IC(50)=113.7 micromol/L for COX-1; IC(50)=25.8 micromol/L for COX-2). Following oral administration of the drug, maximal ex vivo inhibitions were 56% (COX-1) and 83% (COX-2). Acetaminophen plasma concentrations remained above the in vitro IC(50) for COX-2 for at least 5 h postadministration. Ex vivo IC(50) values (COX-1: 105.2 micromol/L; COX-2: 26.3 micromol/L) of acetaminophen compared favorably with its in vitro IC(50) values[3]. Moreover, detrimental effect of APAP (Acetaminophen) on cell viability was suppressed in the presence of HV110 (Lactobacillus fermentum BGHV110 strain) which was linked with increased conversion of LC3 protein and p62/SQSTM1 protein degradation. Additionally, higher p62/SQSTM1 and PINK1 mRNA transcription were noticed in cells co-treated with APAP/HV110, simultaneously[4]. Acetaminophen is a hormone disrupter (ie, it interferes with sex and thyroid hormone function essential for normal brain development) and thus may not be considered a safe drug during pregnancy[5].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00377364 Asthma Rheuma... 展开 >>tic Disease 收起 << Phase 4 Completed - United States, Texas ... 展开 >> UT Southwestern Medical Center at Dallas Dallas, Texas, United States, 75390 收起 <<
NCT01827475 - Completed - -
NCT00377364 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

6.62mL

1.32mL

0.66mL

33.08mL

6.62mL

3.31mL

66.16mL

13.23mL

6.62mL
参考文献

[1]Vad NM, Yount G, et al. Biochemical mechanism of acetaminophen (APAP) induced toxicity in melanoma cell lines. J Pharm Sci. 2009 Apr;98(4):1409-25.

[2]Simmons DL, Botting RM, et al. Induction of an acetaminophen-sensitive cyclooxygenase with reduced sensitivity to nonsteroid antiinflammatory drugs. Proc Natl Acad Sci U S A. 1999 Mar 16;96(6):3275-80.

[3]Hinz B, Cheremina O, Brune K. Acetaminophen (paracetamol) is a selective cyclooxygenase-2 inhibitor in man. FASEB J. 2008;22(2):383-390

[4]Dinić M, Lukić J, Djokić J, et al. Lactobacillus fermentum Postbiotic-induced Autophagy as Potential Approach for Treatment of Acetaminophen Hepatotoxicity. Front Microbiol. 2017;8:594. Published 2017 Apr 6

[5]Aminoshariae A, Khan A. Acetaminophen: old drug, new issues. J Endod. 2015;41(5):588-593