| Size | Price | Stock | Qty |
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| 500mg |
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| 1g |
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| 2g |
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| 5g |
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| 10g |
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| 25g |
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| 50g |
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Purity: ≥98%
Oxaprozin (Oxaprozinum, DL-8280, WY-21743; DR-3355, Hoe-280, ORF-28489, Ru-43280, Tarivid) is a potent nonsteroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic properties. It is also an inhibitor of COX-1 and COX-2 enzymes with IC50s of 2.2 μM and 36 μM for human platelet COX-1 and IL-1-stimulated human synovial cell COX-2, respectively. Oxaprozin has been approved for use in the treatment of RA-rheumatoid arthritis, OA-osteoarthritis, dysmenorrhea, and to alleviate moderate pain. The anti-inflammatory activity of Oxaprozin is due to inhibition of COX-cylooxygenase in platelets, which results in the blockage of prostaglandin synthesis. Oxaprozin shows lower COX-2 selectivity implying higher COX-1 selectivity.
| ln Vitro |
Apoptosis is induced by oxiprozin in a dose-dependent way. When caspase-3 is engaged, oxaprozin boosts its activity; however, when it is at rest, it does not. Oxaprozin at 50 μM inhibits the activation of NF-κB. When the reagent IκBα activates the IKK system, oxaprozin prevents it from happening[1]. The highest proapoptotic effect is induced by oxaprozin (100 μM), which also greatly promotes the apoptosis of CD40L-treated monocytes. Treatment with oxiprozin prevents Akt and NF-κB (p65) phosphorylation that is triggered by CD40L[2].
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| ln Vivo |
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| Animal Protocol |
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| References |
[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.
[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 |
| Molecular Formula |
C18H15NO3
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| Molecular Weight |
293.32
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| CAS # |
21256-18-8
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| Related CAS # |
Oxaprozin-d4;Oxaprozin potassium;174064-08-5;Oxaprozin-d5
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| SMILES |
O1C(C([H])([H])C([H])([H])C(=O)O[H])=NC(C2C([H])=C([H])C([H])=C([H])C=2[H])=C1C1C([H])=C([H])C([H])=C([H])C=1[H]
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| InChi Key |
GSDSWSVVBLHKDQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H20FN3O4/c1-10-9-26-17-14-11(16(23)12(18(24)25)8-22(10)14)7-13(19)15(17)21-5-3-20(2)4-6-21/h7-8,10H,3-6,9H2,1-2H3,(H,24,25)
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| Chemical Name |
9-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-3,7-dihydro-2H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.52 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.52 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.52 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.3409 mL | 1.7046 mL | 3.4092 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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