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4-乙酰氨基酚 /Acetaminophen {[allProObj[0].p_purity_real_show]}

货号:A660637 同义名: 对乙酰氨基酚;N-(4-羟基苯基)乙酰胺 / Paracetamol;4-Acetamidophenol

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

Acetaminophen 化学结构 CAS号:103-90-2
Acetaminophen 化学结构
CAS号:103-90-2
Acetaminophen 3D分子结构
CAS号:103-90-2
Acetaminophen 化学结构 CAS号:103-90-2
Acetaminophen 3D分子结构 CAS号:103-90-2
规格 价格 会员价 库存 数量
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Acetaminophen 纯度/质量文件 产品仅供科研

货号:A660637 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 COX COX-1 COX-2 其他靶点 纯度
Piroxicam 98%
Salicylic acid 98%
Phenacetin 98%
Etodolac 99%
Flunixin meglumine 98%
Ibuprofen L-lysine 99%
Nabumetone 98%
Acemetacin 98%
Diflunisal 98%
Pranoprofen 98%
Ampiroxicam 98%
Meloxicam 98%
Sulindac 98%
Ketoprofen 98%
Mefenamic Acid 95%
Bromfenac sodium 98%
Oxaprozin 99%
Aspirin 99%
Nepafenac 98%
Zaltoprofen 99%
Salicin 98%
Suprofen 99%+
Xanthohumol 99%
Parecoxib 98%
Tolfenamic Acid +++

COX-2, IC50: 0.2 μM

98%
Etoricoxib 99%
Niflumic Acid 98%
Valdecoxib ++++

COX-2, IC50: 5 nM

99+%
Ibuprofen +

COX-1, IC50: 13 μM

+

COX-2, IC50: 370 μM

98%
Indomethacin ++

COX1, IC50: 0.28 μM

+

COX-2, IC50: 14 μM

97%
Lornoxicam ++++

COX-1, IC50: 5 nM

++++

COX-2, IC50: 8 nM

98%
Meclofenamic acid sodium ++++

COX-1, IC50: 40 nM

+++

COX-2, IC50: 50 nM

99%
Rofecoxib ++++

COX-2, IC50: 18 nM

98%
Asaraldehyde 98%
Naproxen +

COX-1, IC50: 8.7 μM

+

COX-2, IC50: 5.2 μM

98%
Diclofenac Sodium Salt +++

COX-1, IC50: 60 nM

+++

COX-2, IC50: 200 nM

98%
NS-398 ++

COX-2, IC50: 3.8 μM

98%
Amfenac Sodium Hydrate ++

COX-1, IC50: 250 nM

+++

COX-2, IC50: 150 nM

98%+
Nimesulide +

COX-2, IC50: 26 μM

98%
Lumiracoxib ++

COX-1, Ki: 3 μM

+++

COX-2, Ki: 60 nM

98%
Rutaecarpine 95%
Celecoxib ++++

COX-2, IC50: 40 nM

98%
Carprofen ++++

canine COX2, IC50: 30 nM

98%
Ketorolac ++

COX-1 (human), IC50: 1.23 μM

++

COX-2 (human), IC50: 3.50 μM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Acetaminophen 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].

Acetaminophen 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 - -

Acetaminophen 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

Acetaminophen 实验方案

计算器
存储液制备 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

Acetaminophen 技术信息

CAS号103-90-2
分子式C8H9NO2
分子量 151.16
别名 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
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature

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
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