| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Meloxicam-13C6 targets the cyclooxygenase (COX) enzymes, specifically COX-2 and COX-1. As an isotope-labeled version of meloxicam, it retains the same pharmacological activity: inhibition of COX-2 (IC50 = 0.49 uM) and COX-1 (IC50 = 36.6 uM). COX-2 is the inducible isoform responsible for prostaglandin synthesis at sites of inflammation, and its inhibition mediates the anti-inflammatory, analgesic, and antipyretic effects of NSAIDs. COX-1 is constitutively expressed and its inhibition contributes to gastrointestinal side effects. Meloxicam is a preferential COX-2 inhibitor. The 13C6 label does not alter binding affinity or selectivity. However, as an analytical standard, it is not used for pharmacological studies.
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| ln Vitro |
In vitro, Meloxicam-13C6 has the same activity as unlabeled meloxicam: it inhibits COX-1 and COX-2 with IC50 values of 36.6 uM and 0.49 uM, respectively. It inhibits prostaglandin E2 (PGE2) production in LPS-stimulated macrophages. In whole blood assays, it inhibits COX-2 more potently than COX-1. However, as a stable isotope-labeled internal standard, Meloxicam-13C6 is not used for in vitro pharmacological studies; it is used for bioanalytical method development. It is added to biological samples (at trace concentrations, typically 10-100 ng/mL) to serve as an internal standard for LC-MS/MS quantification of unlabeled meloxicam. At these trace concentrations, it has no biological activity.
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| ln Vivo |
Meloxicam-13C6 is not used for in vivo pharmacological studies. As an internal standard, it is not administered to animals. Unlabeled meloxicam is widely used in vivo as an NSAID. In rodent models of inflammation (e.g., carrageenan-induced paw edema, adjuvant-induced arthritis), meloxicam (1-10 mg/kg, oral or IP) reduces edema, pain, and fever. Meloxicam-13C6 is used as an internal standard to measure meloxicam concentrations in pharmacokinetic studies of meloxicam. It is added to plasma or tissue samples before extraction. No in vivo activity of the labeled compound is studied. It is for research use only.
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| Enzyme Assay |
Meloxicam-13C6 is not used in cell-free enzyme assays as an inhibitor; it is used as an internal standard in bioanalysis. For cell-free COX inhibition assays, unlabeled meloxicam is used. A typical COX inhibition assay: incubate 10 nM recombinant COX-1 or COX-2 with 10 uM arachidonic acid and varying concentrations of meloxicam (0.001-1000 uM) in assay buffer. After 10 minutes, the reaction is stopped, and PGE2 is measured by EIA. The IC50 values are determined. Meloxicam-13C6 is used as an internal standard in the LC-MS/MS method for quantifying meloxicam in these in vitro samples. In the LC-MS/MS method, Meloxicam-13C6 (50 ng/mL) is added to samples. The mass spectrometer monitors transitions: for meloxicam, m/z 352 → 115; for meloxicam-13C6, m/z 358 → 115 (shift of +6). The peak area ratio is used for quantification. This cell-free analytical method ensures accurate measurement.
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| Cell Assay |
Meloxicam-13C6 is not used directly in cell culture experiments. It may be used as an internal standard when measuring meloxicam concentrations in cell culture media or cell lysates from cells treated with unlabeled meloxicam. A typical cellular assay for meloxicam activity: RAW 264.7 macrophages are seeded in 24-well plates (1 × 10⁵ cells/well). Cells are stimulated with LPS (1 ug/mL) for 24 hours, with or without meloxicam (0.1-100 uM). PGE2 levels in the supernatant are measured by ELISA. Meloxicam-13C6 is not added to the cells; it is added during the sample preparation for confirmatory LC-MS/MS analysis if needed. The labeled compound is an analytical standard, not a treatment.
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| Animal Protocol |
Meloxicam-13C6 is not administered in vivo. Unlabeled meloxicam is used in animal studies. A typical in vivo protocol for meloxicam in a rat PK study: male Sprague-Dawley rats (250-300 g) receive a single oral dose of meloxicam (5 mg/kg) in 0.5% methylcellulose. Blood samples (0.3 mL) are collected from the jugular vein at 0, 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72 hours post-dose. Plasma is separated. Meloxicam-13C6 (50 ng/mL) is added to each plasma sample as an internal standard. Proteins are precipitated with acetonitrile, and the supernatant is analyzed by LC-MS/MS. Calibration curves are prepared using blank plasma spiked with meloxicam (1-1000 ng/mL) and a fixed concentration of Meloxicam-13C6. The concentration of meloxicam in study samples is determined from the peak area ratio. This protocol is standard for bioanalysis of meloxicam. The labeled compound is critical for accurate PK quantification.
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| ADME/Pharmacokinetics |
Meloxicam-13C6 has a molecular weight of 357.34 (the free base of unlabeled meloxicam is 351.41; the +6 Da shift comes from 6 13C atoms). The compound is a white to off-white solid. It is soluble in DMSO (50 mg/mL) and moderately soluble in ethanol. For storage: powder at -20degC. Protect from light. It is stable for at least 2 years. As an internal standard, it is typically prepared as a 1 mg/mL stock solution in DMSO, then diluted in acetonitrile or mobile phase to a working concentration of 10-100 ng/mL. It is used only in analytical methods. Not for human use.
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| Toxicity/Toxicokinetics |
Meloxicam-13C6 is a stable isotope-labeled compound and has the same safety profile as unlabeled meloxicam if ingested or inhaled. However, it is used only in analytical applications at trace concentrations, so the risk is minimal. Standard safety precautions: wear gloves, lab coat, safety glasses. Avoid inhalation of dust. Not for human consumption. Dispose of as chemical waste. The unlabeled meloxicam has an oral LD50 in rats >5000 mg/kg and is known to cause gastrointestinal irritation and renal toxicity at high doses. However, these are not relevant for the labeled compound.
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| References |
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| Additional Infomation |
Meloxicam-13C6 has CAS number not listed (the labeled compound). The unlabeled meloxicam CAS is 71125-38-7. Meloxicam-13C6 is also known as Meloxicam-13C6, a stable isotope. It contains 13C6 labeling. Purity >98%. Research applications: bioanalysis, pharmacokinetic studies, bioequivalence studies, and LC-MS/MS method development for meloxicam. For research use only. Storage: powder at -20degC.
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| Molecular Formula |
C813C6H13N3O4S2
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| Molecular Weight |
357.36
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| Related CAS # |
Meloxicam; 71125-38-7
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| Appearance |
Solid powder
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7983 mL | 13.9915 mL | 27.9830 mL | |
| 5 mM | 0.5597 mL | 2.7983 mL | 5.5966 mL | |
| 10 mM | 0.2798 mL | 1.3991 mL | 2.7983 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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