Molecular Weight(MW): 206.28
Ibuprofen (Dolgesic) is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50 of 13 μM and 370 μM, respectively.
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|Description||Ibuprofen (Dolgesic) is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50 of 13 μM and 370 μM, respectively.|
|Features||Considered a core medicine in the WHO's "WHO Model List of Essential Medicines" (a list of the minimum medical requirements for a basic healthcare system).|
Ibuprofen works by inhibiting the enzyme cyclooxygenase COX-1 and COX-2, which convert arachidonic acid to prostaglandin H2 (PGH2). Its action is similar to aspirin, indomethacin and all other NSAIDs in intact cells, broken cells, and purified enzyme preparations.  Ibuprofen inhibits the constitutive activation of NF-κB and IKKα in the androgen-independent prostate tumor cells PC-3 and DU-145. It sensitizes prostate cells to ionizing radiation and blocks stimulated activation of NF-κB following exposure to TNFα or ionizing radiation in the androgen-sensitive prostate tumor cell line LNCaP. Both of these cannot be attributed directly to inhibition of IκB-α kinase but to inhibition of an upstream regulator of IKKα.  Ibuprofen exerts an anticancer effect by reducing survival of cancer cells. Ibuprofen is more efficacious than aspirin and acetaminophen, and comparable with (R)-flurbiprofen and indomethacin in induction of p75NTR protein (a tumor and metastasis suppressor) expression in cell lines from bladder and other organs. 
|In vivo||Ibuprofen reacts with the heme group of cyclooxygenase to prevent arachidonic acid conversion. Prior exposure to Ibuprofen in vivo protects cyclooxygenase completely from the irreversible effects of aspirin in platelets.  Ibuprofen treatment is effective in attenuating joint inflammation and early articular cartilage degeneration in the adult female Sprague-Dawley rat model induced by high-repetition and high-force (HRHF) task. It dose this by blocking the increases in serum C1 and 2C (a biomarker of collagen I and II degradation) as well as the ratio of collagen degradation to synthesis (C1, 2C/CPII, the latter a biomarker of collage type II synthesis) induced by HRHF. |
Radiochemical enzyme assays for COX-1 and COX-2:10 μL of purified COX-1 (0.7-0.8 μg) or COX-2 (3.0 units, 0.3μg) is activated with 50 μL of cofactor solution [l-epinephrine (1.3 mg/mL), reduced glutathione (0.3 mg/mL), and hematin (1.3 mg/mL) in oxygen-free Tris-HCl buffer (pH 8.0)]. The enzyme solution (60 μL) is added to Ibuprofen solutions or DMSO (20 μL) after [14C]arachidonic acid is added in 0.2 mL eight-strip test tubes and preincubated 10 minutes on ice. Samples are incubated for 15 minutes at 37 °C, after which the reaction is terminated by addition of 10 μL of 2 M HCl and 5 μL of carrier solution (PGE2 and PGF2α, 0.2 μg/mL of each in EtOH). The unmetabolized arachidonic acid is separated from the prostaglandin products by column chromatography and eluted with n-hexane-dioxane-glacial acetic acid (70:30:1). The prostaglandin products are then eluted with EtOAc-MeOH (85:15), and the samples are counted in a Packard scintillation spectrometer. IC50 values are obtained by linear regression analysis.
-  Noreen Y, et al. J Nat Prod, 1998, 61(1), 2-7.
-  Palayoor ST, et al. Oncogene, 1999, 18(51), 7389-7394.
-  Khwaja F, et al. Cancer Res, 2004, 64(17), 6207-6213.
|In vitro||DMSO||41 mg/mL (198.75 mM)|
|Ethanol||41 mg/mL (198.75 mM)|
|In vivo||Add solvents individually and in order:
1% DMSO+30% polyethylene glycol+1% Tween 80
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02689063||Recruiting||Post Operative Pain||AFT Pharmaceuticals, Ltd.||October 26, 2016||Phase 3|
|NCT02904304||Not yet recruiting||Cold||Ache Laboratorios Farmaceuticos S.A.||January 2018||Phase 3|
|NCT02985177||Not yet recruiting||Emergency Service, Hospital|Child/Adolescent Problem|Acute Pain|Fentanyl|Ibuprofen|Analgesics, Opioid|Anti-inflammatory Agents, Non-steroidal||St. Justines Hospital||October 2017||Phase 4|
|NCT02656914||Not yet recruiting||Flu Symptoms||EMS||July 2017||Phase 3|
|NCT02656888||Not yet recruiting||Flu Symptoms||EMS||July 2017||Phase 3|
|NCT02956525||Not yet recruiting||Healthy Volunteers||Apsen Farmaceutica S.A.||June 2017||Phase 1|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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