1. Immunology/Inflammation
  2. COX
  3. Ketoprofen

Ketoprofen (RP-19583) is a non-steroidal anti-inflammatory agent. Ketoprofen can inhibits the activity of cyclooxygenase with IC50 values of 2 nM (COX-1) and 26 nM (COX-2). which is potential in the research of inflammation, immunology, and metabolic disease such as obesity.

For research use only. We do not sell to patients.

CAS No. : 22071-15-4

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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500 mg In-stock
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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of Ketoprofen:

Top Publications Citing Use of Products

    Ketoprofen purchased from MedChemExpress. Usage Cited in: Eur J Pharm Sci. 2023 Oct 1:189:106550.  [Abstract]

    Binding constants for ENC and BINI to HSA derived from fluorescence quenching data obtained at 25 °C in the absence and presence of IND, Ketoprofen, HEM.

    View All COX Isoform Specific Products:

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Ketoprofen (RP-19583) is a non-steroidal anti-inflammatory agent. Ketoprofen can inhibits the activity of cyclooxygenase with IC50 values of 2 nM (COX-1) and 26 nM (COX-2). which is potential in the research of inflammation, immunology, and metabolic disease such as obesity[1][2][3].

    IC50 & Target[1]

    COX-1

    2 nM (IC50, in human blood monocytes)

    COX-2

    26 nM (IC50, in human blood monocytes)

    Cellular Effect
    Cell Line Type Value Description References
    A549 IC50
    > 50 μM
    Compound: Ketoprofen
    Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
    Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
    [PMID: 32987314]
    A549 IC50
    > 50 μM
    Compound: Ketoprofen
    Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
    Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
    [PMID: 32987314]
    A549 IC50
    > 50 μM
    Compound: Ketoprofen
    Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
    Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
    [PMID: 32987314]
    CHO IC50
    1.3 μM
    Compound: Ketoprofen
    TP_TRANSPORTER: inhibition of Adefovir uptake in OAT1-expressing CHO cells
    TP_TRANSPORTER: inhibition of Adefovir uptake in OAT1-expressing CHO cells
    [PMID: 10991954]
    CHO IC50
    1.4 μM
    Compound: Ketoprofen
    TP_TRANSPORTER: inhibition of 6-Carboxyfluorescein uptake in OAT1-expressing CHO cells
    TP_TRANSPORTER: inhibition of 6-Carboxyfluorescein uptake in OAT1-expressing CHO cells
    [PMID: 10929807]
    DU-145 IC50
    > 100 μM
    Compound: 5; Ket
    Antiproliferative activity against human DU-145 cells incubated for 48 hrs by MTT assay
    Antiproliferative activity against human DU-145 cells incubated for 48 hrs by MTT assay
    [PMID: 36257283]
    HT-29 IC50
    > 100 μM
    Compound: 5; Ket
    Antiproliferative activity against human HT-29 cells incubated for 48 hrs by MTT assay
    Antiproliferative activity against human HT-29 cells incubated for 48 hrs by MTT assay
    [PMID: 36257283]
    HeLa IC50
    > 50 μM
    Compound: Ketoprofen
    Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
    Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
    [PMID: 32987314]
    HeLa IC50
    > 50 μM
    Compound: Ketoprofen
    Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
    Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
    [PMID: 32987314]
    HeLa IC50
    > 50 μM
    Compound: Ketoprofen
    Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
    Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
    [PMID: 32987314]
    MCF7 IC50
    > 100 μM
    Compound: 5; Ket
    Antiproliferative activity against human MCF7 cells incubated for 48 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells incubated for 48 hrs by MTT assay
    [PMID: 36257283]
    MCF7 IC50
    > 50 μM
    Compound: Ketoprofen
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
    [PMID: 32987314]
    MCF7 IC50
    > 50 μM
    Compound: Ketoprofen
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
    [PMID: 32987314]
    MCF7 IC50
    > 50 μM
    Compound: Ketoprofen
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
    [PMID: 32987314]
    Oocyte IC50
    0.5 μM
    Compound: Ketoprofen
    TP_TRANSPORTER: inhibition of MTX uptake in Xenopus laevis oocytes
    TP_TRANSPORTER: inhibition of MTX uptake in Xenopus laevis oocytes
    [PMID: 11099697]
    RAW264.7 IC50
    7.07 μM
    Compound: Ketoprofen
    Antiinflammatory activity in LPS-induced mouse RAW264.7 cells assessed as inhibition of NO production pretreated for 1 hr followed by LPS stimulation and measured after 24 hrs by griess reagent based assay
    Antiinflammatory activity in LPS-induced mouse RAW264.7 cells assessed as inhibition of NO production pretreated for 1 hr followed by LPS stimulation and measured after 24 hrs by griess reagent based assay
    [PMID: 38286094]
    SW480 IC50
    > 50 μM
    Compound: Ketoprofen
    Cytotoxicity against human SW480 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
    Cytotoxicity against human SW480 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
    [PMID: 32987314]
    SW480 IC50
    > 50 μM
    Compound: Ketoprofen
    Cytotoxicity against human SW480 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
    Cytotoxicity against human SW480 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
    [PMID: 32987314]
    SW480 IC50
    > 50 μM
    Compound: Ketoprofen
    Cytotoxicity against human SW480 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
    Cytotoxicity against human SW480 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
    [PMID: 32987314]
    In Vitro

    Ketoprofen inhibits COX in LPS-stimulated monocytes isolated from human blood, with IC50 values of 2 nM (COX-1) and 26 nM (COX-2)[1].
    Ketoprofen (2.5 mg /mL, 3-24h) decreases the mRNA level of immune factors (TNFα, IL-8, SAA and COX-2) and PTGES in LPS-stimulated bovine mammary epithelial cells[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    RT-PCR[3]

    Cell Line: LPS (0.2 μg/mL)-stimulated bovine mammary epithelial cells
    Concentration: 2.5 mg /mL
    Incubation Time: 3, 6, 24 h
    Result: Decreased the mRNA level of TNFα, IL-8, SAA, COX-2 and PTGES.
    In Vivo

    Ketoprofen (Oral administration, 10 mg/kg, three times a week for 10 weeks, HFD-induced obese C57BL/6 mice) decreases in relative body weight (15.41%), the iWAT mass (approximately 41%), and leptin (58.68%) and resistin (12.88%)[2].
    Ketoprofen (50 mg/kg, LPS-treated dairy cows) lowers the increase of somatic cell count (SCC), serum albumin (SA), IgG and lactate dehydrogenase (LDH) activity in milk induced by LPS[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: HFD-induced obese C57BL/6 mice[2]
    Dosage: 10 mg/kg
    Administration: Oral administration, three times a week for 10 weeks
    Result: Decreased in relative body weight, the iWAT mass, and the level of leptin and resistin.
    Animal Model: LPS (0.2 μg/mL)-treated dairy cows [3]
    Dosage: 50 mg/kg
    Administration: Injection (Milk samples were taken every 30 min until 6 and 9 h)
    Result: Lowered the increase of somatic cell count (SCC), serum albumin (SA), IgG and lactate dehydrogenase (LDH) activity in milk.
    Molecular Weight

    254.28

    Formula

    C16H14O3

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C1=CC=CC=C1)C2=CC=CC(C(C(O)=O)C)=C2

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (393.27 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (9.83 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (9.83 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.95%

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.9327 mL 19.6634 mL 39.3267 mL 98.3168 mL
    5 mM 0.7865 mL 3.9327 mL 7.8653 mL 19.6634 mL
    10 mM 0.3933 mL 1.9663 mL 3.9327 mL 9.8317 mL
    15 mM 0.2622 mL 1.3109 mL 2.6218 mL 6.5545 mL
    20 mM 0.1966 mL 0.9832 mL 1.9663 mL 4.9158 mL
    25 mM 0.1573 mL 0.7865 mL 1.5731 mL 3.9327 mL
    30 mM 0.1311 mL 0.6554 mL 1.3109 mL 3.2772 mL
    40 mM 0.0983 mL 0.4916 mL 0.9832 mL 2.4579 mL
    50 mM 0.0787 mL 0.3933 mL 0.7865 mL 1.9663 mL
    60 mM 0.0655 mL 0.3277 mL 0.6554 mL 1.6386 mL
    80 mM 0.0492 mL 0.2458 mL 0.4916 mL 1.2290 mL
    100 mM 0.0393 mL 0.1966 mL 0.3933 mL 0.9832 mL
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