产品说明书

Ibuprofen

Print
Chemical Structure| 15687-27-1 同义名 : 2-(4-异丁基苯基)丙酸 ;DL-Ibuprofen;NSC 256857;Ibuprofen, Advil, Motrin, Nurofen, Brufen;U-18753;(±)-Ibuprofen
CAS号 : 15687-27-1
货号 : A238702
分子式 : C13H18O2
纯度 : 98%
分子量 : 206.28
MDL号 : MFCD00010393
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(509.02 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
动物实验配方：

1% DMSO+30% polyethylene glycol+1% Tween 80+water 20 mg/mL suspension

生物活性
靶点

  • COX-2

    COX-2, IC50:370 μM

  • COX-1

    COX-1, IC50:13 μM
描述 Cyclooxygenase (COX) is an enzyme that mainly contains a house-keeping enzyme COX-1 and an inducible cyclooxygenase COX-2. COX-1 is expressed throughout the body and important for gastrointestinal protection while the expression of COX-2 is related to cytokines, growth factors and other inflammatory ulcerogenic stimuli[1]. Ibuprofen, which is one of the most widely used analgesic-antipyretic-anti-inflammatory drugs today, is a COX inhibitor with IC50 value of 2.7 μM for COX-1 and 1.8 μM for COX-2[2]. In the COX-2 inhibitory assay based on the inhibition potential of conversion of arachidonic acid to prostaglandin H2 by human recombinant COX-2, Ibuprofen was prepared at a concentration of 50 μg/ml and the COX-2 inhibitory activity was 57.3% [3] .
In carrageenan-induced rat paw dedma model of wistar albino rat, 20 mg/kg by weight of ibuprofen was administered orally. The paw volume of the rat was measured at hourly interval for 3 h (0, 1, 2 and 3 h) and the percent inhibition of edema was 65.9% [4] . For the analgesic activity experiment, acetic acid induced writhing method on swiss CD1 mice was used. 10 mg/kg, 20 mg/kg and 70 mg/kg of Ibuprofen was given to the mice orally and the inhibition of analgesic activity after 30 mins was 48%, 53% and 67%, respectively[5].
作用机制 COX enzymes oxygenate polyunsaturated fatty acids to prostaglandin endoperoxides and then generate prostaglandins and thromboxanes. Ibuprofen is weak, competitive inhibitors of COX-2 oxygenation of arachidonic acid and potent, noncompetitive inhibitor of 2-arachidonoylglycerol oxygenation[6].
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
NCT01530217 Inflammation ... 展开 >>Pulpitis 收起 << Not Applicable Completed - -
NCT02294019 Patient Compliance Phase 3 Completed - United States, Alabama ... 展开 >> Robert's Discount Pharmacy Hoover, Alabama, United States, 35226 Pharmacy at the Pig McCalla, Alabama, United States, 35111 United States, Arizona Community Clinical Pharmacy Mesa, Arizona, United States, 85202 United States, Florida Garden Drug Fort Lauderdale, Florida, United States, 33309 Pill Box Pharmacy and Medical Supply Pembroke Pines, Florida, United States, 33026 Summerfield Pharmacy Riverview, Florida, United States, 33569 United States, Georgia Sutton Family Pharmacy Dalton, Georgia, United States, 30721 Wynn's Pharmacy Inc. Griffin, Georgia, United States, 30224 United States, Minnesota Goodrich Pharmacy Andover, Minnesota, United States, 55304 Goodrich Pharmacy Anoka, Minnesota, United States, 55303 Goodrich Pharmacy Blaine, Minnesota, United States, 55434 Goodrich Pharmacy Elk River, Minnesota, United States, 55330 Cub Pharmacy Number 1924 St. Louis Park, Minnesota, United States, 55426 United States, Missouri Albers' Specialty Pharmacy Kansas City, Missouri, United States, 64111 Countryside Pharmacy Savannah, Missouri, United States, 64485 United States, New Jersey Texas Road Pharmacy Monroe, New Jersey, United States, 08831 United States, New Mexico Phil's Pills, Inc. Albuquerque, New Mexico, United States, 87110 Total Health and Wellness Center of Taos Taos, New Mexico, United States, 87571 United States, North Carolina Kroger Pharmacy #342 Cary, North Carolina, United States, 27513 United States, Pennsylvania Family Prescription Center Bethlehem, Pennsylvania, United States, 18015 United States, Utah The Medicine Shoppe Bountiful, Utah, United States, 84010 Northview Pharmacy Layton, Utah, United States, 84041 Family Plaza Pharmacy West Jordan, Utah, United States, 84088 United States, Washington Foothills Compounding Pharmacy Enumclaw, Washington, United States, 98022 Ostrom Drugs Kenmore, Washington, United States, 98028 收起 <<
NCT03523988 NSAID Pain Ma... 展开 >>nagement 收起 << Phase 4 Completed - United States, Washington ... 展开 >> University of Washington Seattle, Washington, United States, 98195 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.85mL

0.97mL

0.48mL

24.24mL

4.85mL

2.42mL

48.48mL

9.70mL

4.85mL
参考文献

[1]Hawkey CJ. COX-1 and COX-2 inhibitors. Best Pract Res Clin Gastroenterol. 2001;15(5):801-20.

[2]Vitale P, Panella A, et al. COX-1 Inhibitors: Beyond Structure Toward Therapy. Med Res Rev. 2016;36(4):641-71.

[3]Theoduloz C, Alzate-Morales J, et al. Inhibition of key enzymes in the inflammatory pathway by hybrid molecules of terpenes and synthetic drugs: In vitro and in silico studies. Chem Biol Drug Des. 2019;93(3):290-299.

[4]Kaur A, Pathak DP, et al. Synthesis, biological evaluation and docking study of N-(2-(3,4,5-trimethoxybenzyl)benzoxazole-5-yl) benzamide derivatives as selective COX-2 inhibitor and anti-inflammatory agents. Bioorg Chem. 2018.

[5]Navarro L, Rosell G, et al. Synthesis and biological properties of aryl methyl sulfones. Bioorg Med Chem. 2018;26(14):4113-4126.

[6]Prusakiewicz JJ, Duggan KC, et al. Differential sensitivity and mechanism of inhibition of COX-2 oxygenation of arachidonic acid and 2-arachidonoylglycerol by ibuprofen and mefenamic acid. Biochemistry. 2009;48(31):7353-5.