Home Neuronal Signaling COX inhibitor Ibuprofen (NSC 256857) For research use only.

Ibuprofen (NSC 256857)

Synonyms: Dolgesic,NSC 256857

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

Ibuprofen (NSC 256857) Chemical Structure

Ibuprofen (NSC 256857) Chemical Structure

CAS: 15687-27-1

Selleck's Ibuprofen (NSC 256857) has been cited by 7 publications

Purity & Quality Control

Batch: S163801 DMSO] 41 mg/mL] false] Ethanol] 41 mg/mL] false] Water] Insoluble] false Purity: 100%
100

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Signaling Pathway

COX Signaling Pathways

COX Signaling Pathway

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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
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]
Kinase Assay 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 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.
In Vivo
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]
Animal Research 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
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06146491 Recruiting
Pain Postoperative
B.P. Koirala Institute of Health Sciences
 August 10 2023 Phase 4
NCT05928520 Not yet recruiting
Pain Management
Al-Azhar University
 August 1 2023 Phase 3
NCT05575700 Recruiting
Pain Acute|Hip Arthropathy|Knee Arthropathy|Safety Issues|Analgesia|Analgesic Adverse Reaction|Postoperative Pain|Postoperative Complications
Naestved Hospital
 April 17 2023 Phase 4
NCT05496868 Recruiting
Acute Respiratory Distress Syndrome Adult
Dompé Farmaceutici S.p.A
 February 7 2023 Phase 2
NCT05674721 Completed
Pain
HALEON
 January 5 2023 Phase 1

Chemical Information & Solubility

Molecular Weight 206.28 Formula

C13H18O2
CAS No. 15687-27-1 SDF Download Ibuprofen (NSC 256857) SDF
Smiles CC(C)CC1=CC=C(C=C1)C(C)C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 41 mg/mL ( (198.75 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 41 mg/mL

Water : Insoluble


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In vivo
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