Ibuprofen (NSC 256857)

Catalog No.S1638 Batch:S163801

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Technical Data

Formula

C13H18O2
Molecular Weight 206.28 CAS No. 15687-27-1
Solubility (25°C)* In vitro DMSO 41 mg/mL (198.75 mM)
Ethanol 41 mg/mL (198.75 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO Corn oil
2.5mg/ml Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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.
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]
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).

Protocol (from reference)

Kinase Assay:[1]
  • 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 Assay:[3]
  • 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.
Animal Study:[5]
  • 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

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

Characterization of pain-related behaviors and gene expression profiling of peripheral sensory ganglia in a mouse model of acute ankle sprain [ Front Behav Neurosci, 2023, 17:1189489] PubMed: 37304762
Febrile Temperature Critically Controls the Differentiation and Pathogenicity of T Helper 17 Cells. [ Immunity, 2020, 52(2):328-341] PubMed: 32049050
Ibuprofen induces ferroptosis of glioblastoma cells via downregulation of nuclear factor erythroid 2-related factor 2 signaling pathway. [ Anticancer Drugs, 2020, 31(1):27-34] PubMed: 31490283
The Establishment and Validation of the Human U937 Cell Line as a Cellular Model to Screen Immunomodulatory Agents Regulating Cytokine Release Induced by Influenza Virus Infection [ Virol Sin, 2019, 34(6):648-661] PubMed: 31286365
A network integration approach for drug-target interaction prediction and computational drug repositioning from heterogeneous information. [ Nat Commun, 2017, 8(1):573] PubMed: 28924171
Repurposing FDA-approved drugs for anti-aging therapies. [ Biogerontology, 2016, 17(5-6):907-920] PubMed: 27484416
PDE5 inhibitors enhance celecoxib killing in multiple tumor types. [ J Cell Physiol, 2015, 230(5):1115-27] PubMed: 25303541

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SHIPPING AND STORAGE
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