Ketoprofen [22071-15-4]

Referentie HY-B0227-1g

Formaat : 1g

Merk : MedChemExpress


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]
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]
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]
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.
Masse moléculaire

254.28

Formule

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

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvant et solubilité
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.

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.
Pureté et documentation
Références

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