| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
Glucocorticoid receptor (GR); acts as a GR agonist.
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| ln Vitro |
Drug compounds have included stable heavy isotopes of carbon, hydrogen, and other elements, mostly as quantitative tracers while the drugs were being developed. Because deuteration may have an impact on a drug's pharmacokinetics and metabolic profile, it has drawn attention [1].
Dexamethasone significantly reduces CD11b, CD18, and CD62L expression on neutrophils and CD11b/CD18 expression on monocytes; it inhibits LPS-induced exosomal inflammatory miRNA-155 production in macrophages. |
| ln Vivo |
Dexamethasone has potent anti-inflammatory and immunosuppressive activity in vivo; it is used for allergies, inflammation, and COVID-19 research; the d3-labeled analog has identical pharmacodynamics.
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| Enzyme Assay |
Receptor binding is assessed by competitive binding assays using [3H]-dexamethasone and GR-containing cytosolic preparations; non-specific binding is determined with excess unlabeled dexamethasone.
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| Cell Assay |
Primary human immune cells or cell lines (e.g., THP-1, A549) are treated with 0.1-1000 nM dexamethasone for 1-24 hours; gene expression (NF-kappaB target genes, IL-6, TNF-alpha) is measured by qPCR or ELISA.
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| Animal Protocol |
Dexamethasone is administered intraperitoneally, subcutaneously, or orally at 1-30 mg/kg in mice; anti-inflammatory efficacy is evaluated in carrageenan-induced paw edema, LPS-induced endotoxemia, or collagen-induced arthritis models.
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| ADME/Pharmacokinetics |
As a stable isotope-labeled internal standard, Dexamethasone-d3-1 is used to quantify unlabeled dexamethasone in PK studies; dexamethasone has high oral bioavailability (70-90%) and a plasma half-life of 3-4 hours in humans.
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| Toxicity/Toxicokinetics |
Dexamethasone has well-characterized toxicity including hyperglycemia, immunosuppression, osteoporosis, and adrenal suppression with chronic use; the labeled analog has an identical safety profile.
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| References | |
| Additional Infomation |
Dexamethasone is a WHO Essential Medicine approved for numerous inflammatory and autoimmune conditions; the d3-labeled version is a research-grade analytical standard, not a marketed pharmaceutical.
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| Molecular Formula |
C22H26D3FO5
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|---|---|
| Molecular Weight |
395.48
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5286 mL | 12.6429 mL | 25.2857 mL | |
| 5 mM | 0.5057 mL | 2.5286 mL | 5.0571 mL | |
| 10 mM | 0.2529 mL | 1.2643 mL | 2.5286 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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