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[Medlife优选]对乙酰氨基苯酚 APAP

2024年04月18日 17:18   生物.医药.天然产物  

上海陌孚医药科技有限公司 发布 访问商铺

关键词:对乙酰氨基苯酚 APAP;103-90-2
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。
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]
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Medlife,致力于提供高品质、高性价比小分子化合物的产品。

Medlife小分子化合物大量库存,提供超过2万种的抑制剂、激动剂、拮抗剂等产品,是药物及疾病研究的重要原料供应商。


Medlife小分子化合物大量库存,提供超过2万种的抑制剂、激动剂、拮抗剂等产品,是药物及疾病研究的重要原料供应商。
化工词典
  • 中文名称: 醋氨酚
  • 英文名称: Acetaminophen
  • CAS NO.: 103-90-2
  • 分子式: C8H9NO2
  • 分子量:151.1626
醋氨酚结构式图片|103-90-2结构式图片
查看更多物化属性、结构等信息,点击: 103-90-2
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