2. Immunology/Inflammation
  3. COX
  4. Celecoxib

Celecoxib,a selective non-steroidal anti-inflammatory drug (NSAID), is a selective COX-2 inhibitor with an IC50 of 40 nM.

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Celecoxib Chemical Structure

Celecoxib Chemical Structure

CAS No. : 169590-42-5

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Customer Review

Based on 37 publication(s) in Google Scholar

Other Forms of Celecoxib:

Celecoxib Related Antibodies

Top Publications Citing Use of Products

34 Publications Citing Use of MCE Celecoxib

WB

    Celecoxib purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2018 Jan;118(2):213-223.  [Abstract]

    Western blotting of EP2, EP4, COX-2, and PTEN using proteins extracted from SVHUC cells without MCA exposure and MCA-exposed SVHUC cells subsequently cultured for 6 weeks with ethanol or Celecoxib (1 mM). GAPDH served as a loading control.

    Celecoxib purchased from MedChemExpress. Usage Cited in: Sci Rep. 2018 Mar 7;8(1):4108.  [Abstract]

    L02 cells exposed to PA (200 μM) with different concentrations of Celecoxib (Cel, 5-40 μM) for 24 h. Celecoxib decreases protein expression of COX-2 compared with control as indicated by western blot.

    Celecoxib purchased from MedChemExpress. Usage Cited in: Oncol Rep. 2018 Oct;40(4):2242-2250.  [Abstract]

    Effects of Gefitinib(G) and Celecoxib(Cel) on ABCB1 (MDR1), FOXM1 and Bcl 2 protein levels in PC3/DR and DU145/DR cell lines. The effects of Gefitinib, Celecoxib and their combination on ABCB1 (MDR1), FOXM1 and Bcl 2 expression in the PC3/DR and DU145/DR cell lines are determined by a western blot assay.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Celecoxib,a selective non-steroidal anti-inflammatory drug (NSAID), is a selective COX-2 inhibitor with an IC50 of 40 nM.

    IC50 & Target[1]

    COX-2

    40 nM (IC50)

    COX-1

    15 μM (IC50)

    In Vitro

    The selective cyclooxygenase-2 (COX-2) inhibitor Celecoxib (10-75 μM) inhibits the proliferation of the NPC cell lines in a dose-dependent manner. Celecoxib (25 and 50 μM) induces apoptosis and cell-cycle arrest at the G0/G1 checkpoint in the NPC cell lines, which is associated with significantly reduced STAT3 phosphorylation. The genes downstream of STAT3 (ie, Survivin, Mcl-1, Bcl-2 and Cyclin D1) are significantly down-regulated after exposure to Celecoxib (25 and 50 μM)[2].
    Targeting the YAP/TAZ transcriptional target cyclooxygenase 2 (COX-2) using celecoxib inhibits cell proliferation and tumorigenesis in NF2 mutant cells[6].

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

    Celecoxib Related Antibodies
    In Vivo

    Celecoxib demonstrates potent, oral anti-inflammatory activity. Celecoxib reduces acute inflammation in the carrageenan edema assay with an ED50 of 7.1 mg/kg and reduces chronic inflammation in the adjuvant arthritis model with an ED50 of 0.37 mg/kg/day. In addition, Celecoxib also exhibits analgesic activity in the Hargreaves hyperalgesia model with an ED50 of 34.5 mg/kg. Celecoxib has potency equivalent to that of standard nonsteroidal anti-inflammatory drugs (NSAIDs), yet shows no acute GI toxicity in rats at doses up to 200 mg/kg. In addition, it displays no chronic GI toxicity in rats at doses up to 600 mg/kg/day over 10 days[1]. In the KpB mice fed a high fat diet (obese) and treated with Celecoxib, tumor weight decreases by 66% when compare with control animals. Among KpB mice fed a low fat diet (non-obese), tumor weight decreases by 46% after treatment with Celecoxib[3]. Rat models are orally administrated with Celecoxib (20 mg/kg) and/or intramuscularly with Fasudil (10 mg/kg) for 2 weeks. Results demonstrates that the combined use of Celecoxib and fasudil significantly decreases COX-2 and Rho kinase II expression surrounding the lesion site in rats with spinal cord injury, improves the pathomorphology of the injured spinal cord, and promoted the recovery of motor function[4].

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

    381.37

    Formula

    C17H14F3N3O2S
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CC1=CC=C(C=C1)C2=CC(C(F)(F)F)=NN2C3=CC=C(C=C3)S(=O)(N)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 50 mg/mL (131.11 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.6221 mL 13.1106 mL 26.2213 mL
    5 mM 0.5244 mL 2.6221 mL 5.2443 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

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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 (6.56 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 (6.56 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
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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    (per animal)

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    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
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    %
    Saline
    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
    References
    Cell Assay
    [2]

    The antiproliferative effect of Celecoxib on NPC cells is assessed using an MTT assay. Cells are seeded into 96-well plates and allowed to attach for 24 h. The cells are then treated with increasing concentrations of Celecoxib (0, 5, 10, 25, 50 or 75 μM) dissolved in DMSO (final concentration ≤0.1%) and incubated for up to 48 h. After the incubation, 20 μL of MTT dye (5 mg/mL) are added to each well and cells are incubated at 37°C for 4 h. After removing the supernatants, the crystals are dissolved in DMSO and the absorbance is measured at 490 nm. The percentage growth inhibition is calculated as (ODcontrol−ODdrug)/ODcontrol×100%. The half-maximal inhibitory concentration (IC50) values and the 95% confidence intervals are calculated using probit regression using SPSS 15.0 software. The experiment is performed in triplicate and repeated at least three times[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [3][4]

    Mice[3]
    The KpB mice are monitored weekly by palpation for tumor growth. Celecoxib and placebo treatment is initiated after palpation of a 1 cm tumor in mice on the HFD (obese group) and LFD (non-obese group) (N=15 mice per group). Celecoxib is dissolved in DMSO at 5 mg/mL, further diluted 10 times in 0.5% methylcellulose with 0.025% Tween 80 and injected (IP) daily at a dose of 5 mg/kg body weight for 4 weeks. The tumor sizes are measured once a week by palpation. Tumor volume is calculated using the following equation: volume (mm3)=a×b2/2, where is the largest diameter and b is the smallest diameter. The animals are weighed weekly throughout the study. At sacrifice, mice are weighed and blood samples are taken. Half of the ovarian tumor is snap-frozen and stored at −80°C, and the other half is fixed in 10% neutral-buffered formalin and paraffin embedded. Mouse heart, lungs and kidneys are also harvested, fixed in formalin and grossly examined for any suspicious lesions before paraffin embedding.
    Rats[4]
    Forty adult, clean, female, Sprague-Dawley rats aged 3 months and weighing 280-330 g, are used. Forty rats are randomized to five groups as follows: sham surgery, model, Celecoxib, fasudil and combination groups, with eight rats in each group. Rats in the Celecoxib group are intragastrically administrated with a suspension of Celecoxib (20 mg/kg), and a suspension of Celecoxib containing 0.5% sodium carboxymethylcellulose is made from the capsules. Rats in the fasudil group are intramuscularly administrated with fasudil hydrochloride injection (10 mg/kg) via the dorsal muscle. Rats in the combination group are administrated with both a suspension of Celecoxib (20 mg/kg) and fasudil hydrochloride (10 mg/kg). The fasudil and Celecoxib doses are based on doses administered to adults and these are adjusted in a pre-study. Administration is once every day for 2 weeks. Subsequently, all rats are treated normally for another 2 weeks, and then sacrificed either for histological examination or for western blot assay.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.6221 mL 13.1106 mL 26.2213 mL 65.5531 mL
    5 mM 0.5244 mL 2.6221 mL 5.2443 mL 13.1106 mL
    10 mM 0.2622 mL 1.3111 mL 2.6221 mL 6.5553 mL
    15 mM 0.1748 mL 0.8740 mL 1.7481 mL 4.3702 mL
    20 mM 0.1311 mL 0.6555 mL 1.3111 mL 3.2777 mL
    25 mM 0.1049 mL 0.5244 mL 1.0489 mL 2.6221 mL
    30 mM 0.0874 mL 0.4370 mL 0.8740 mL 2.1851 mL
    40 mM 0.0656 mL 0.3278 mL 0.6555 mL 1.6388 mL
    50 mM 0.0524 mL 0.2622 mL 0.5244 mL 1.3111 mL
    60 mM 0.0437 mL 0.2185 mL 0.4370 mL 1.0926 mL
    80 mM 0.0328 mL 0.1639 mL 0.3278 mL 0.8194 mL
    100 mM 0.0262 mL 0.1311 mL 0.2622 mL 0.6555 mL
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    Celecoxib Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Celecoxib169590-42-5SC 58635SC58635SC-58635COXCyclooxygenaseInhibitorinhibitorinhibit

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