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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%
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。

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。

*
搜索质检报告(COA)

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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