1. Immunology/Inflammation
  2. COX
  3. NS-398

NS-398 is a non-steroidal an-inflammatory agent with analgesic and antipyretic effects, and selectively inhibits prostaglandin G/H synthase 2/cyclooxygenase 2 (COX-2) activity, with an IC50 of 3.8 μM, and has no effect on COX-1 at 100 μM.

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NS-398 Chemical Structure

NS-398 Chemical Structure

CAS No. : 123653-11-2

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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USD 61 In-stock
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10 mM * 1 mL in DMSO USD 61 In-stock
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Customer Review

Based on 18 publication(s) in Google Scholar

Top Publications Citing Use of Products

    NS-398 purchased from MedChemExpress. Usage Cited in: Mol Med Rep. 2019 Oct;20(4):3811-3819.  [Abstract]

    Expression of E-cadherin and vimentin is regulated by COX‑2. MG‑63 cells are infected with control or COX-2-overexpressing lentivirus, and treated with or without the COX‑2 inhibitor NS398 or the PI3K inhibitor LY294002. (A) The expression of E-cadherin (green) in each group was determined using immunofluorescence. (B) Quantification of E‑cadherin expression.

    NS-398 purchased from MedChemExpress. Usage Cited in: Mol Med Rep. 2019 Oct;20(4):3811-3819.  [Abstract]

    Expression of NF‑κB p65 protein is regulated by COX‑2. MG‑63 cells were infected with control or COX‑2‑overexpressing lentivirus, and treated with or without the COX‑2 inhibitor NS398 or the PI3K inhibitor LY294002. (A)The expression of NF-κB p65 (green) in each group was determined by immunofluorescence. (B) Quantification of NF-κB p65 expression.

    NS-398 purchased from MedChemExpress. Usage Cited in: Mol Med Rep. 2019 Oct;20(4):3811-3819.  [Abstract]

    Expression of E-cadherin and vimentin is regulated by COX‑2. MG‑63 cells are infected with control or COX-2-overexpressing lentivirus, and treated with or without the COX‑2 inhibitor NS398 or the PI3K inhibitor LY294002. (C) The expression of vimentin in each group. (D) Quantification of vimentin expression.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    NS-398 is a non-steroidal an-inflammatory agent with analgesic and antipyretic effects, and selectively inhibits prostaglandin G/H synthase 2/cyclooxygenase 2 (COX-2) activity, with an IC50 of 3.8 μM, and has no effect on COX-1 at 100 μM.

    IC50 & Target[1]

    COX-2

    3.8 μM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    A549 IC50
    20 μM
    Compound: 1, NS-398
    Inhibition of mPGES-1 in human A549 cell microsomes assessed as conversion of PGH2 into PGE2 at 0 degC after 5 mins by HPLC-UV analysis
    Inhibition of mPGES-1 in human A549 cell microsomes assessed as conversion of PGH2 into PGE2 at 0 degC after 5 mins by HPLC-UV analysis
    [PMID: 22209272]
    HaCaT IC50
    10 nM
    Compound: NS-398
    Inhibition of PGE2 production in human HaCaT cells after 24 hrs by RIA
    Inhibition of PGE2 production in human HaCaT cells after 24 hrs by RIA
    [PMID: 15387642]
    RAW264.7 IC50
    > 10 μM
    Compound: NS-398
    Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as nitrite accumulation after 20 hrs by fluorimetry
    Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as nitrite accumulation after 20 hrs by fluorimetry
    [PMID: 11678654]
    RAW264.7 IC50
    0.007 μM
    Compound: NS-398
    Inhibition of mPGES-1 in mouse RAW264.7 cells assessed as reduction in LPS-induced PGE2 production after 24 hrs
    Inhibition of mPGES-1 in mouse RAW264.7 cells assessed as reduction in LPS-induced PGE2 production after 24 hrs
    [PMID: 27720548]
    RAW264.7 IC50
    0.007 μM
    Compound: NS-398
    Inhibition of COX-2 in mouse RAW264.7 cells assessed as decrease in LPS-induced PGE2 production treated prior to LPS challenge by enzyme immunoassay
    Inhibition of COX-2 in mouse RAW264.7 cells assessed as decrease in LPS-induced PGE2 production treated prior to LPS challenge by enzyme immunoassay
    [PMID: 24656662]
    RAW264.7 IC50
    0.00723 μM
    Compound: NS-398
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced PGE2 production after 24 hrs by enzyme immunoassay
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced PGE2 production after 24 hrs by enzyme immunoassay
    [PMID: 29107425]
    RAW264.7 IC50
    0.05 μM
    Compound: NS-398
    Inhibition of COX2-mediated PGE2 production in LPS-stimulated mouse RAW264.7 cells by enzyme immunoassay
    Inhibition of COX2-mediated PGE2 production in LPS-stimulated mouse RAW264.7 cells by enzyme immunoassay
    [PMID: 19233646]
    RAW264.7 IC50
    0.1 μM
    Compound: NS-398
    Inhibition of IFN-gamma/LPS-induced PGE2 production in mouse RAW264.7 cells after 17 to 20 hrs by EIA method
    Inhibition of IFN-gamma/LPS-induced PGE2 production in mouse RAW264.7 cells after 17 to 20 hrs by EIA method
    [PMID: 25027933]
    RAW264.7 IC50
    0.81 μM
    Compound: NS-398
    Inhibition of COX2 in mouse RAW264.7 cells by enzyme immunoassay
    Inhibition of COX2 in mouse RAW264.7 cells by enzyme immunoassay
    [PMID: 20056549]
    RAW264.7 IC50
    2.1 μM
    Compound: NS-398
    Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as PGE2 accumulation after 20 hrs by RIA
    Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as PGE2 accumulation after 20 hrs by RIA
    [PMID: 11678654]
    RAW264.7 IC50
    4.8 μM
    Compound: NS-398
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced PGE2 production by EIA
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced PGE2 production by EIA
    [PMID: 20004572]
    RAW264.7 IC50
    6.7 nM
    Compound: NS-398
    Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as decrease in PGE2 production preincubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA
    Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as decrease in PGE2 production preincubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA
    [PMID: 31747281]
    RAW264.7 IC50
    6.74 μM
    Compound: NS398
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-stimulated PGE2 production by ELISA
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-stimulated PGE2 production by ELISA
    [PMID: 28408221]
    RAW264.7 IC50
    63.7 μM
    Compound: NS-398
    Inhibition of COX1 in mouse RAW264.7 cells by enzyme immunoassay
    Inhibition of COX1 in mouse RAW264.7 cells by enzyme immunoassay
    [PMID: 20056549]
    RAW264.7 IC50
    7 nM
    Compound: NS-398
    Suppression of PGE2 production in LPS-induced mouse RAW264.7 cells after 24 hrs by enzyme immunoassay
    Suppression of PGE2 production in LPS-induced mouse RAW264.7 cells after 24 hrs by enzyme immunoassay
    [PMID: 26602278]
    RAW264.7 IC50
    7.01 nM
    Compound: NS398
    Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced PGE2 production administered 1 hr prior to LPS-challenge measured after 24 hrs by EIA
    Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced PGE2 production administered 1 hr prior to LPS-challenge measured after 24 hrs by EIA
    [PMID: 24360561]
    RAW264.7 IC50
    7.23 nM
    Compound: NS-398
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced PGE2 production pretreated for 1 hr followed by LPS addition measured after 24 hrs
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced PGE2 production pretreated for 1 hr followed by LPS addition measured after 24 hrs
    [PMID: 29102229]
    SK-BR-3 IC50
    0.68 μM
    Compound: 1
    Inhibition of aromatase in human SKBR3 cells by tritiated water release assay
    Inhibition of aromatase in human SKBR3 cells by tritiated water release assay
    [PMID: 18271519]
    SK-BR-3 IC50
    0.72 μM
    Compound: 2e
    Cytotoxicity against human SK-BR-3 cells after 24 hrs by MTT assay relative to NS398
    Cytotoxicity against human SK-BR-3 cells after 24 hrs by MTT assay relative to NS398
    [PMID: 17095221]
    In Vitro

    NS-398 is a non-steroidal an-inflammatory agent, selectively inhibits prostaglandin G/H synthase/cyclooxygenase (COX-2) activity, with an IC50 of 3.8 μM, and has no effect on COX-1 at 100 μM[1]. NS-398 weakly inhibits PG endoperoxide synthase activity from sheep seminal vesicle microsomes (IC50, 11 μM)[2].

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

    In Vivo

    NS-398 (0.5-10 mg/kg, p.o.) dose-dependently inhibits paw edema in rats, with an ED30 of 1.14 mg/kg, shows therapeutic effects on adjuvant arthritis (ED30, 4.69 mg/kg), exhibits dose-dependent analgesic activity (ED50, 1.65 mg/kg), and has antipyretic effect (ED50, 1.84 mg/kg) in rats. In mice, NS-398 suppresses writhing reactions induced by acetic acid with an ED50 of 8.2 mg/kg[2].

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

    Molecular Weight

    314.36

    Formula

    C13H18N2O5S

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    CS(=O)(NC1=CC=C([N+]([O-])=O)C=C1OC2CCCCC2)=O

    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 : 33.33 mg/mL (106.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.1811 mL 15.9053 mL 31.8107 mL
    5 mM 0.6362 mL 3.1811 mL 6.3621 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.

    • 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)

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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    90% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (7.95 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      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.
    • Protocol 2

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

      Solubility: ≥ 1.67 mg/mL (5.31 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    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 +
    +
    %
    Tween-80 +
    %
    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
    Animal Administration
    [2]

    Mice[2]
    Briefly, male ddy mice weighing about 30 g are used. The writhing syndrome is induced by injecting 0.75% of acetic acid, intraperitoneally. Ten minutes later, the number of writhings are counted for the next 10 min. NS-398 is administered orally 30 min prior to the injection. The analgesic effect is expressed as % of inhibition, compared with the vehicle-treated control[2].
    Rats[2]
    Briefly, male Lewis rats weighing about 160 g are used. Arthritis is induced by injecting 0.1 mL of 0.7% Mycobacterium tubercu-losis-liquid paraffin into the left hind paw. On day 15, the rats are grouped according to the degree of secondary lesions in the right hind paw. NS-398 is administered orally once daily from days 15 to 18. Foot volume is measured on day 19. Relative edema volume (REV) is calculated for each animal[2].

    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, 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 3.1811 mL 15.9053 mL 31.8107 mL 79.5267 mL
    5 mM 0.6362 mL 3.1811 mL 6.3621 mL 15.9053 mL
    10 mM 0.3181 mL 1.5905 mL 3.1811 mL 7.9527 mL
    15 mM 0.2121 mL 1.0604 mL 2.1207 mL 5.3018 mL
    20 mM 0.1591 mL 0.7953 mL 1.5905 mL 3.9763 mL
    25 mM 0.1272 mL 0.6362 mL 1.2724 mL 3.1811 mL
    30 mM 0.1060 mL 0.5302 mL 1.0604 mL 2.6509 mL
    40 mM 0.0795 mL 0.3976 mL 0.7953 mL 1.9882 mL
    50 mM 0.0636 mL 0.3181 mL 0.6362 mL 1.5905 mL
    60 mM 0.0530 mL 0.2651 mL 0.5302 mL 1.3254 mL
    80 mM 0.0398 mL 0.1988 mL 0.3976 mL 0.9941 mL
    100 mM 0.0318 mL 0.1591 mL 0.3181 mL 0.7953 mL
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    Cat. No.:
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