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Purity: ≥98%
Ketoprofen (formerly RP 19583; RP-19583; Ketoprofen, Profenid, Orudis, Alrheumun, Capisten) is a potent nonsteroidal anti-inflammatory drugs (NSAID), acting as a dual COX1/2 inhibitor with potential anti-inflammatory activity. It was approved as a nonsteroidal anti-inflammatory drug to treat arthritis-related inflammatory pains. Ketoprofen combined with UVB irradiation induces the cytotoxicity and suppresses DNA synthesis in HaCaT cells in a concentration-dependent manner. Ketoprofen combined with UVB irradiation inhibits the cell growth and induces G2/M cell cycle arrest by modulating the levels of cdc2, cyclin B1, Chk1, Tyr15-phosphorylated cdc2 and p21.
ln Vitro |
In LPS-stimulated monocytes isolated from human blood, ketoprofen inhibits COX with IC50 values of 2 nM (COX-1) and 26 nM (COX-2)[1]. In LPS-stimulated bovine mammary epithelial cells, ketoprofen (2.5 mg/mL, 3–24 hours) reduces the mRNA level of immune factors (TNFα, IL-8, SAA, and COX-2) and PTGES[3].
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ln Vivo |
In HFD-induced obese C57BL/6 mice, ketoprofen (oral treatment, 10 mg/kg, three times a week for 10 weeks) reduces relative body weight (15.41%), iWAT mass (about 41%), and the levels of leptin (58.68%) and resistin (12.88%)[2]. In dairy cows exposed with lipopolysaccharide (LPS), ketoprofen (50 mg/kg) reduces the rise in somatic cell count (SCC), serum albumin (SA), immunoglobulin G (IgG), and lactate dehydrogenase (LDH) activity in milk[3].
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Cell Assay |
RT-PCR[3]
Cell Types: LPS (0.2 μg/mL)-stimulated bovine mammary epithelial cells Tested Concentrations: 2.5 mg /mL Incubation Duration: 3, 6, 24 h Experimental Results: diminished the mRNA level of TNFα, IL-8, SAA, COX-2 and PTGES. |
Animal Protocol |
Animal/Disease Models: HFD-induced obese C57BL/6 mice[2]
Doses: 10 mg/kg Route of Administration: Oral administration, three times a week for 10 weeks Experimental Results: diminished in relative body weight, the iWAT mass, and the level of leptin and resistin. Animal/Disease Models: LPS (0.2 μg/mL)-treated dairy cows [3] Doses: 50 mg/kg Route of Administration: Injection (Milk samples were taken every 30 min until 6 and 9 h ) Experimental Results: Lowered the increase of somatic cell count (SCC), serum albumin (SA), IgG and lactate dehydrogenase (LDH) activity in milk. |
References |
[1]. Palomer A, et al. Structure-based design of cyclooxygenase-2 selectivity into ketoprofen. Bioorg Med Chem Lett. 2002 Feb 25;12(4):533-7.
[2]. NamHyeon Kang Ketoprofen alleviates diet-induced obesity and promotes white fat browning in mice via the activation of COX-2 through mTORC1-p38 signaling pathway. Pflugers Arch. 2020 May;472(5):583-596. [3]. Denisa Dan, et al. Ketoprofen affects the mammary immune response in dairy cows in vivo and in vitro. J Dairy Sci. 2018 Dec;101(12):11321-11329. |
Molecular Formula |
C16H14O3
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Molecular Weight |
254.28
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CAS # |
22071-15-4
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Related CAS # |
Ketoprofen-d3;159490-55-8;Ketoprofen-d4;1219805-29-4;S-(+)-Ketoprofen;22161-81-5;Ketoprofen (lysinate);57469-78-0;Ketoprofen-13C,d3;1189508-77-7;Dexketoprofen (trometamol);156604-79-4
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O([H])C(C([H])(C([H])([H])[H])C1C([H])=C([H])C([H])=C(C(C2C([H])=C([H])C([H])=C([H])C=2[H])=O)C=1[H])=O
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.83 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.83 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (9.83 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.9327 mL | 19.6634 mL | 39.3267 mL | |
5 mM | 0.7865 mL | 3.9327 mL | 7.8653 mL | |
10 mM | 0.3933 mL | 1.9663 mL | 3.9327 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT04678076 | Completed | Drug: Ketoprofen Lysine Drug: Ketoprofen Oral Product |
Healthy | Aziende Chimiche Riunite Angelini Francesco S.p.A | July 23, 2018 | Phase 1 |
NCT03514810 | Completed | Combination Product: Combined Sertraline & Ketoprofen Other: Interleukins in MDD after treatment |
Major Depressive Disorder | Kufa University | January 10, 2017 | Phase 1 |
NCT02730026 | Completed | Drug: Ketoprofen Drug: Ketoprofen and Omeprazole |
Pain Other Surgical Procedures |
Luis Fernando Simoneti | June 2015 | Phase 4 |
NCT02350296 | Completed Has Results | Drug: KSL 40 mg Drug: OKi® 80 mg | Pain Disorders | Dompé Farmaceutici S.p.A | November 26, 2014 | Phase 1 |
NCT02491879 | Unknown † | Drug: Ketoprofen Other: Placebo |
Mechanical Low Back Pain | Akdeniz University | June 2015 | Phase 4 |