Ibuprofen (NSC 256857)

For research use only.

Catalog No.S1638 Synonyms: Dolgesic

6 publications

Ibuprofen (NSC 256857) Chemical Structure

CAS No. 15687-27-1

Ibuprofen (NSC 256857, Dolgesic) is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50 of 13 μM and 370 μM, respectively.

Selleck's Ibuprofen (NSC 256857) has been cited by 6 publications

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Biological Activity

Description Ibuprofen (NSC 256857, 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).
Targets
COX-1 [1] COX-2 [1]
13 μM 370 μM
In vitro

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. [1] 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. [2] 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. [3]

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. [4] 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. [5]

Protocol

Kinase Assay:[1]
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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.
Cell Research:[3]
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  • Cell lines: Bladder epithelial cell line T24, RT-4 transitional cell papilloma bladder cell line, 5637 primary carcinoma bladder cell line, HCT-116, MDAMB231, MCF7, HEK293, A549, SKOV3 and DU145
  • Concentrations: Dissolved in DMSO at a concentration of 200 mM for making the stock solution, final concentration ~2 mM
  • Incubation Time: 48 hours
  • Method: Each cell line is incubated with Ibuprofen of various concentrations for 48 hours. Cell survival is estimated by the MTT assay, and cell death is determined by Hoechst staining used to distinguish between intact cell nuclei and fragmented nuclei undergoing cell death. Cells are lysed and analyzed by western blotting for detection of the p75NTR protein.
    (Only for Reference)
Animal Research:[5]
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  • Animal Models: Female Sprague-Dawley rats with joint inflammation induced by high-repetition and high-force (HRHF) tasks
  • Dosages: 45 mg/kg
  • Administration: Taken orally every day
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 41 mg/mL (198.75 mM)
Water Insoluble
Ethanol '41 mg/mL
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% DMSO+30% polyethylene glycol+1% Tween 80
For best results, use promptly after mixing.
20 mg/mL

* 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.

Chemical Information

Molecular Weight 206.28
Formula

C13H18O2

CAS No. 15687-27-1
Storage powder
in solvent
Synonyms Dolgesic
Smiles CC(C)CC1=CC=C(C=C1)C(C)C(=O)O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05013567 Not yet recruiting Drug: Ibuprofen gel|Other: Placebo Musculoskeletal Pain|Acute Pain|Stretch|Sprains Brainfarma Industria Química e Farmacêutica S/A March 2022 Phase 3
NCT04986839 Not yet recruiting Drug: Paracetamol injection|Drug: Ibuprofen injection Patent Ductus Arteriosus Manchester University NHS Foundation Trust October 1 2021 Phase 2|Phase 3
NCT05030324 Not yet recruiting Drug: XC221 100 mg|Drug: XC221 200 mg|Drug: Placebo Influenza|Viral Respiratory Infection|Acute Viral Upper Respiratory Infections Valenta Pharm JSC September 2021 Phase 2
NCT04942015 Not yet recruiting Drug: Honghuaruyi Wan|Drug: Placebo of Honghuaruyi Wan Endometriosis|Dysmenorrhea Beijing University of Chinese Medicine June 21 2021 Phase 4
NCT04723394 Active not recruiting Drug: AZD7442|Drug: Placebo COVID-19 AstraZeneca January 28 2021 Phase 3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID