2. Immunology/Inflammation NF-κB PI3K/Akt/mTOR Apoptosis
  3. COX NF-κB Akt IKK Apoptosis
  4. Oxaprozin

Oxaprozin  (Synonyms: Oxaprozinum; Wy21743)

Cat. No.: HY-B0808 Purity: 99.95%
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Oxaprozin is an orally active and potent COX inhibitor, with IC50 values of 2.2 μM for human platelet COX-1 and and 36 μM for IL-1-stimulated human synovial cell COX-2, respectively. Oxaprozin also inhibits the activation of NF-κB. Oxaprozin induces cell apoptosis. Oxaprozin shows anti-inflammatory activity. Oxaprozin-mediated inhibition of the Akt/IKK/NF-κB pathway contributes to its anti-inflammatory properties.

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Oxaprozin Chemical Structure

Oxaprozin Chemical Structure

CAS No. : 21256-18-8

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Oxaprozin:

Oxaprozin Related Antibodies

Top Publications Citing Use of Products

View All COX Isoform Specific Products:

View All Isoforms
COX COX-1 COX-2 COX-3

View All NF-κB Isoform Specific Products:

View All Isoforms
NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

View All Akt Isoform Specific Products:

View All Isoforms
Akt Akt1 Akt2 Akt3

View All IKK Isoform Specific Products:

View All Isoforms
IKK-α IKK-β IKK IKKε TBK1

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Oxaprozin is an orally active and potent COX inhibitor, with IC50 values of 2.2 μM for human platelet COX-1 and and 36 μM for IL-1-stimulated human synovial cell COX-2, respectively. Oxaprozin also inhibits the activation of NF-κB. Oxaprozin induces cell apoptosis. Oxaprozin shows anti-inflammatory activity. Oxaprozin-mediated inhibition of the Akt/IKK/NF-κB pathway contributes to its anti-inflammatory properties[1][2].

IC50 & Target[1]

COX-1

2.2 μM (IC50)

COX-2

36 μM (IC50)

NF-κB

 

IKK

 

In Vitro

Oxaprozin induces apoptosis in a dose-dependent manner. Oxaprozin increases caspase-3 activity in the activated but not in the resting condition. NF-κB activation is inhibited by Oxaprozin (50 μM). Oxaprozin inhibits activation of the IKK system induced by the reagent IκBα[1].
Oxaprozin (100 μM) induces the strongest proapoptotic effect and significantly increases CD40L-treated monocyte apoptosis. Oxaprozin treatment inhibits CD40L-induced Akt and NF-κB (p65) phosphorylation[2].

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

Oxaprozin Related Antibodies
Clinical Trial
Molecular Weight

293.32

Formula

C18H15NO3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)CCC1=NC(C2=CC=CC=C2)=C(C3=CC=CC=C3)O1
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 (340.92 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 3.4092 mL 17.0462 mL 34.0925 mL
5 mM 0.6818 mL 3.4092 mL 6.8185 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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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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 (8.52 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 (8.52 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

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
Kinase Assay
[2]

Caspase 3 activity in the presence or absence of 200 ng/mL CD40L plus 1 μg/mL CD40L enhancer and 100 μM Oxaprozin is performed. The enzymatic activity is spectrophotometrically determined for 60 minutes at 405 nm assuming an extinction coefficient of 8.8×103 M1/cm[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[2]

Purified monocytes are resuspended at 106/mL and cultured for 48 hours. In selective experiments, cells are cultured in the presence or absence of 50 μM PD98059, 1 μM SB203580, 50 μM LY294002, 20 μM SN-50, 50 μM Ac-DEVD-CHO, different doses (5, 10, 50, 100 μM) of Oxaprozin, 100 μM ibuprofen,100 μM indomethacin, or 100 μM naproxene. Percentages of apoptotic cells are measured by both fluorescence microscope and flow cytometer[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 3.4092 mL 17.0462 mL 34.0925 mL 85.2311 mL
5 mM 0.6818 mL 3.4092 mL 6.8185 mL 17.0462 mL
10 mM 0.3409 mL 1.7046 mL 3.4092 mL 8.5231 mL
15 mM 0.2273 mL 1.1364 mL 2.2728 mL 5.6821 mL
20 mM 0.1705 mL 0.8523 mL 1.7046 mL 4.2616 mL
25 mM 0.1364 mL 0.6818 mL 1.3637 mL 3.4092 mL
30 mM 0.1136 mL 0.5682 mL 1.1364 mL 2.8410 mL
40 mM 0.0852 mL 0.4262 mL 0.8523 mL 2.1308 mL
50 mM 0.0682 mL 0.3409 mL 0.6818 mL 1.7046 mL
60 mM 0.0568 mL 0.2841 mL 0.5682 mL 1.4205 mL
80 mM 0.0426 mL 0.2131 mL 0.4262 mL 1.0654 mL
100 mM 0.0341 mL 0.1705 mL 0.3409 mL 0.8523 mL
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Oxaprozin 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:

Oxaprozin21256-18-8Oxaprozinum Wy21743Wy21743Wy 21743Wy-21743COXNF-κBAktIKKApoptosisCyclooxygenaseNuclear factor-κBNuclear factor-kappaBPKBProtein kinase BIκB kinaseI kappa B kinase NSAIDapoptosisanti-inflammatoryInhibitorinhibitorinhibit

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