| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Oxaprozin-d4 targets the cyclooxygenase (COX) enzymes, specifically COX-1 and COX-2, which are key enzymes in the biosynthesis of prostaglandins. By inhibiting these enzymes, the parent compound Oxaprozin reduces the production of prostaglandins, which are inflammatory mediators responsible for pain, fever, and swelling. The deuterated form is chemically identical to the parent drug in terms of target engagement and pharmacological activity, but it is used exclusively as an analytical standard. The deuterium labeling does not alter the mechanism of action.
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| ln Vitro |
No specific in vitro activity data is available for Oxaprozin-d4 itself because it is an analytical standard, not a pharmacological test compound. The parent compound Oxaprozin has demonstrated potent COX inhibitory activity in vitro. In cell-free COX enzyme assays, Oxaprozin inhibits ovine COX-1 and human recombinant COX-2 with IC50 values of approximately 2.2 microM and 36 microM, respectively, indicating moderate selectivity for COX-1. In whole blood assays (reflecting in vivo COX inhibition), the IC50 for thromboxane B2 (TxB2) production is ∼9.9 microM. These enzyme inhibition properties underlie the anti-inflammatory, analgesic, and antipyretic effects of the drug.
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| ln Vivo |
No specific in vivo data is available for the deuterated form. The parent compound Oxaprozin has been extensively characterized in preclinical and clinical studies. In animal models of inflammation (e.g., carrageenan-induced paw edema in rats), oral administration of Oxaprozin (10-30 mg/kg) produces significant reduction in paw swelling. In the adjuvant-induced arthritis model in rats, Oxaprozin (15-45 mg/kg/day) reduces joint swelling, erythema, and histological damage. The compound is well absorbed following oral administration with an onset of action within 1-2 hours in animal models. These in vivo anti-inflammatory effects are mediated through COX inhibition and reduced prostaglandin synthesis.
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| Enzyme Assay |
Oxaprozin-d4 is not used in cell-free or enzymatic assays for target engagement evaluation. The deuterated standard is employed in analytical method development. For LC-MS/MS method validation, a calibration curve is constructed by spiking known concentrations of non-deuterated Oxaprozin into blank biological matrix (plasma or tissue homogenate). A fixed concentration of Oxaprozin-d4 internal standard (e.g., 100 ng/mL) is added to each calibrator and sample. The ratio of analyte peak area to internal standard peak area is plotted against the nominal concentration. The standard curve range is typically 5-5000 ng/mL. The deuterated standard corrects for matrix effects, recovery variability, and instrument fluctuations.
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| Cell Assay |
Oxaprozin-d4 is not used in cellular assays. For standard cellular assay protocols involving the parent compound, a typical anti-inflammatory assay uses LPS-stimulated RAW 264.7 macrophages. Cells are seeded in 96-well plates at 1×10⁵ cells/well. After 24 hours, Oxaprozin (0.1-100 microM) is added for 2 hours, followed by LPS (1 microg/mL) for 18 hours. Culture supernatants are collected and analyzed for PGE2, TNF-alpha, and IL-6 levels by ELISA. Alternatively, COX-2 protein expression is assessed by Western blotting. Cell viability is measured by MTT assay to exclude cytotoxicity. The deuterated standard is not used in these assays.
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| Animal Protocol |
Oxaprozin-d4 is not administered in vivo as a test compound. For pharmacokinetic studies, the non-deuterated Oxaprozin is administered to animals or human subjects. In a typical rat PK study, male Sprague-Dawley rats (200-250 g) receive a single oral dose of Oxaprozin (10-30 mg/kg) suspended in 0.5% methylcellulose. Blood samples (∼200 microL) are collected via tail vein at pre-dose, 0.25, 0.5, 1, 2, 4, 6, 8, 12, 24, 36, and 48 hours post-dose. Plasma is separated by centrifugation. Oxaprozin-d4 is used as the internal standard for LC-MS/MS quantification of Oxaprozin in plasma samples. Non-compartmental PK parameters (Cmax, Tmax, AUC, t½) are calculated using standard software. This methodology is also used for bioequivalence studies of generic Oxaprozin formulations.
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| ADME/Pharmacokinetics |
Oxaprozin-d4 is a stable, non-radioactive isotope-labeled compound. The lyophilized powder should be stored at -20degC (up to 3 years) or 4degC (up to 2 years) in sealed containers protected from moisture and light. For solution storage, working solutions prepared in DMSO or methanol should be stored at -80degC (6 months) or -20degC (1 month). The compound is soluble in DMSO (typically 10-30 mg/mL) and methanol. For injection formulations in animal studies, the parent compound Oxaprozin can be formulated using 10% DMSO : 5% Tween80 : 85% saline or other suitable vehicles. The deuterated standard is typically used at concentrations of 10-1000 ng/mL in analytical methods.
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| Toxicity/Toxicokinetics |
This product is for research use only and is not for human consumption. No specific toxicity data is available for the deuterated form. The parent compound Oxaprozin has an established safety profile as an approved NSAID. Common adverse effects include gastrointestinal (GI) disturbances, dyspepsia, nausea, and abdominal pain, reflecting COX-1 inhibition in the GI tract. At supratherapeutic doses, Oxaprozin may cause renal toxicity, hepatic injury, and cardiovascular events. The deuterated internal standard is used at minute quantities (ng/mL levels in solutions) that pose negligible risk. Standard laboratory safety practices (gloves, lab coat, safety glasses) should be followed when handling the compound.
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| Additional Infomation |
Oxaprozin (brand name Daypro) is a nonsteroidal anti-inflammatory drug that was approved for the treatment of osteoarthritis and rheumatoid arthritis. It belongs to the propionic acid class of NSAIDs and has a longer plasma half-life (∼40-50 hours in humans) compared to ibuprofen and naproxen, allowing once-daily dosing. Oxaprozin-d4 is a stable isotopic analog where four hydrogen atoms are replaced with deuterium, providing a mass shift of +4 Da. This internal standard is used for accurate quantification in bioanalytical methods. The CAS number for non-deuterated Oxaprozin is 21256-18-8. This product is not an FDA-approved drug; it is a research chemical. Supplier information must not be included.
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| Molecular Formula |
C18H11D4NO3
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| Related CAS # |
Oxaprozin;21256-18-8;Oxaprozin potassium;174064-08-5
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| Appearance |
Typically exists as solid at room temperature
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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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