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对乙酰氨基苯酚 APAP (Synonyms: 对乙酰氨基酚; Paracetamol; 4-Acetamidophenol; 4'-Hydroxyacetanilide)

目录号: PC14299 纯度: ≥99.5%

COX抑制剂，Acetaminophen (paracetamol) 是选择性环氧合酶-2 (COX-2) 的抑制剂，IC50 值为 25.8 μM。它是广泛使用的解热和止痛药。

CAS No. :103-90-2

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中文名称

对乙酰氨基苯酚 APAP

中文别名

对乙酰氨基酚;醋硝香豆素杂质;醋氨酚溶液;对乙酰氨基苯酚,CP;对乙酰胺基苯酚;对乙酰氨基苯酚;4'-羟基乙酰苯胺;4 -羟基乙酰苯胺;4-乙酰氨基苯酚;4-乙酰胺基苯酚;N-(4-羟基苯基)乙酰胺;N-乙酰对氨基酚;醋氨酚;对羟基乙酰苯胺;对十二烷基苯酚;对乙酰氨基苯酚,AR;对乙酰氨基酚 EP标准品;对乙酰氨基酚 USP标准品;对乙酰氨基酚标准品;对乙酰氨基酚-D3;对乙酰氨基酚标准品(JP);对乙酰胺基酚;甘氨酰甘氨酰-L-谷氨酰胺;尼泊金乙酯;扑热息痛;乙酰氨基酚;4-乙酰氨基酚;对醋氨酚;对羟基苯基乙酰胺;分析对照品;退热净;对乙酰氨基酚（4-乙酰氨基酚）;萃酚;百服宁;必理通;斯耐普;索密痛;雅司达;醋氨酚，医药级,纯度:>99%

英文名称

Acetaminophen

英文别名

4-Acetamidophenol;acetaminophen;4-(ACETYLAMINO)PHENOL;4'-HYDROXYACETANILIDE;4-HYDROXYACETANILIDE;ACETYL-P-AMINOPHENOL;APAP;N-(4-HYDROXYPHENYL)ACETAMIDE;N-ACETYL-4-AMINOPHENOL;N-ACETYL-P-AMINOPHENOL;P-ACETAMIDOPHENOL;P-ACETAMINOPHENOL;PARACETAMOL;P-HYDROXYACETANILIDE;RARECHEM AB PP 0382;TYLENOL;4'-Hydroxyacetanilide, paracetamol;Acetaminophen NEW;Acetaminophen solution;ACETAMINOPHEN(P);ACETAMINOPHEN(RG);Paracetamol (Acetaminophen);4-Acetamino phenol;Acetaminophenol;Dirox;Dypap;Exdol;Fevor;G 1;Hedex;Korum;NAPAP;Panex;Somedon;4-acetaminophen;扑热息痛;Acetaminofen;Panadol;Datril;Algotropyl;Naprinol;Lonarid;Anelix;Multin;Acenol;Acamol;Liquagesic;Acetagesic;Pyrinazine;Injectapap;Clixodyne;Servigesic;Acetalgin;Abensanil;Gelocatil;Valgesic;Tussapap;Finimal;Valadol;Tralgon;Tabalgin;Lestemp;Alvedon;Apamide;Paracet;Homoolan;Febrolin;Febrilix;Febridol;Dymad

Cas No.

103-90-2

分子式

C₈H₉NO₂

分子量

151.16

包装储存

Powder	-20°C	3 years
	4°C	2 years

*该产品在溶液状态不稳定，建议您现用现配，即刻使用。

产品详情

COX抑制剂，Acetaminophen (paracetamol) 是选择性环氧合酶-2 (COX-2) 的抑制剂，IC50 值为 25.8 μM。它是广泛使用的解热和止痛药。

生物活性

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. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor.

性状

Solid

IC50 & Target[1][2]

COX-2

25.8 μM (IC₅₀)

COX-1

113.7 μM (IC₅₀)

体外研究(In Vitro)

体外研究, acetaminophen elicites a 4.4-fold selectivity toward COX-2 inhibition (IC₅₀ 113.7 μM for COX-1; IC₅₀ 25.8 μM for COX-2). Following oral administration of the drug, maximal ex vivo inhibitions are 56% (COX-1) and 83% (COX-2). Acetaminophen plasma concentrations remaine above the 体外研究 IC₅₀ for COX-2 for at least 5 h postadministration. Ex vivo IC₅₀ values (COX-1: 105.2 μM; COX-2: 26.3 μM) of acetaminophen compared favorably with its 体外研究 IC₅₀ values. In contrast to previous concepts, acetaminophen inhibited COX-2 by more than 80%, i.e., to a degree comparable to nonsteroidal antiinflammatory drugs (NSAIDs) and selective COX-2 inhibitors. However, a >95% COX-1 blockade relevant for suppression of platelet function is not achieved. MTT assay shows that Acetaminophen (APAP) in a dose of 50 mM significantly (p<0.001) reduces cell viability to 61.5±6.65%. Interestingly, the significant (p<0.01) increase in cell viability to 79.7±2.47% is observed in the Acetaminophen/HV110 co-treated cells, compared to Acetaminophen treated cells.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Administering Acetaminophen (250?mg/kg, orally) to the mice causes significant (p<0.001) liver damage and necrosis of cells as evidenced by the elevated serum hepatic enzymes alanine aminotransferase (ALT), aminotransferase (AST), alkaline phosphatase (ALP), and gamma-glutamyl transferase (γGT) compared with normal group. Conversely, effects of pretreatment with different doses of citral (125, 250, and 500?mg/kg) exhibited a significant (p<0.05) decrease in serum activities of ALT (91.79%, 93.07%, and 95.61%, resp.), AST (93.40%, 91.89%, and 96.52%, resp.), ALP (39.29%, 37.07%, and 59.80%, resp.), and γGT (92.83%, 91.59%, and 93.0%, resp.), when compared to the Acetaminophen group. Similar results were found in pretreatment with SLM on the activity of ALT (95.90%), AST (95.03%), ALP (70.52%), and γGT (92.69%).

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years

*该产品在溶液状态不稳定，建议您现用现配，即刻使用。

ClinicalTrial

参考文献

[1]. Hinz, B, et al. Acetaminophen (paracetamol) is a selective cyclooxygenase-2 inhibitor in man. FASEB J, 2008. 22(2): p. 383-90. [Information]

[2]. Miroslav Dini?, et al. Lactobacillus fermentum Postbiotic-induced Autophagy as Potential Approach for Treatment ofAcetaminophen Hepatotoxicity. Front Microbiol. 2017 Apr 6;8:594. [Information]

[3]. Uchida NS, et al. Hepatoprotective Effect of Citral on Acetaminophen-Induced Liver Toxicity in Mice. Evid Based Complement Alternat Med. 2017;2017:1796209. [Information]

[4]. Rothen JP, et al. Acetaminophen is an inhibitor of hepatic N-acetyltransferase 2 体外研究 and in vivo. Pharmacogenetics. 1998 Dec;8(6):553-9. [Information]

溶解度数据

体外研究:

DMSO : 250 mg/mL (1653.88 mM; Need ultrasonic)

H₂O : 10 mg/mL (66.16 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	6.6155 mL	33.0775 mL	66.1551 mL
5 mM	1.3231 mL	6.6155 mL	13.2310 mL
10 mM	0.6616 mL	3.3078 mL	6.6155 mL

建议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溶液；该产品在溶液状态不稳定，建议您现用现配，即刻使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 0.5% CMC-Na/saline water
Solubility: 10 mg/mL (66.16 mM); Suspended solution; Need ultrasonic
2.

建议依照次序添加每种溶剂： saline 0.5% Tween-80
Solubility: 10 mg/mL (66.16 mM); Clear solution; Need ultrasonic
3.

建议依照次序添加每种溶剂： PBS
Solubility: 6.67 mg/mL (44.13 mM); Clear solution; Need ultrasonic
4.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (13.76 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (13.76 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
5.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (13.76 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (13.76 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
6.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (13.76 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (13.76 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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