Oxaprozin potassium
Oxaprozin potassium 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 potassium also inhibits the activation of NF-κB. Oxaprozin potassium induces cell apoptosis. Oxaprozin potassium shows anti-inflammatory activity. Oxaprozin potassium-mediated inhibition of the Akt/IKK/NF-κB pathway contributes to its anti-inflammatory properties.
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- CAS No.: 174064-08-5
- Formule: C18H14KNO3
- Masse moléculaire:331.41
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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COX-1 2.2 μM (IC50) |
COX-2 36 μM (IC50) |
NF-κB |
IKK |
Oxaprozin (0-100 μM) 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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 174064-08-5
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Masse moléculaire 331.41
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Formule C18H14KNO3
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SMILES
O=C(O[K])CCC1=NC(C2=CC=CC=C2)=C(C3=CC=CC=C3)O1
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Synonyms
Oxaprozinum potassium; Wy21743 potassium
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Ottonello L, et al. Delayed apoptosis of human monocytes exposed to immune complexes is reversed byoxaprozin: role of the Akt/IkappaB kinase/nuclear factor kappaB pathway. Br J Pharmacol. 2009 May;157(2):294-306. [Content Brief]
[2]. Montecucco F, et al. Oxaprozin-induced apoptosis on CD40 ligand-treated human primary monocytes is associated with the modulation of defined intracellular pathways. J Biomed Biotechnol. 2009;2009:478785. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Oxaprozin potassium Related Classifications
HY-B0808A Related Classifications
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