Name: Ibuprofen (NSC 256857)
Brand: Selleck Chemicals
SKU: S1638
Availability: InStock
Rating: 5 (8 reviews)

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

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COA
NMR
HPLC
SDS
Datasheet

100

Related Targets	Adrenergic Receptor AChR 5-HT Receptor Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) GluR
Other COX Products	NS-398 (NS398) Paeoniflorin (NSC 178886) Lumiracoxib Xanthohumol Bufexamac Oroxin B Tolfenamic Acid Nimesulide Ginsenoside Rd Indometacin Sodium

Solubility

In vitro
Batch:

DMSO : 41 mg/mL (198.75 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 41 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.500mg/ml (12.12mM)	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.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

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Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	206.28	Formula	C₁₃H₁₈O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	15687-27-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Dolgesic,NSC 256857			Smiles	CC(C)CC1=CC=C(C=C1)C(C)C(=O)O

Mechanism of Action

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/IC₅₀/Ki	COX-1 13 μM COX-2 370 μM
In vitro	Ibuprofen (NSC 256857) 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. This compound 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. It 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 p75^NTR protein (a tumor and metastasis suppressor) expression in cell lines from bladder and other organs.
Kinase Assay	Radiochemical enzyme assays for COX-1 and COX-2
Kinase Assay	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)]. After [¹⁴C]arachidonic acid is added in 0.2 mL eight-strip test tubes and preincubated 10 minutes on ice, the enzyme solution (60 μL) is added to Ibuprofen (NSC 256857) solutions or DMSO (20 μL). 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.
In vivo	Ibuprofen (NSC 256857) reacts with the heme group of cyclooxygenase to prevent arachidonic acid conversion. Prior exposure to this compound in vivo protects cyclooxygenase completely from the irreversible effects of aspirin in platelets. Its 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 does 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/9461646/ [2] https://pubmed.ncbi.nlm.nih.gov/10602496/ [3] https://pubmed.ncbi.nlm.nih.gov/15342406/ [4] https://pubmed.ncbi.nlm.nih.gov/6411052/ [5] https://pubmed.ncbi.nlm.nih.gov/21403884/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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
NCT06247462	Completed	Acute Kidney Injury	University of New Mexico	June 1 2023	Phase 1
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

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Ibuprofen (NSC 256857) COX inhibitor

Chemical Structure

Molecular Weight: 206.28