| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Cortisone-d8, as an analytical standard, does not bind to any therapeutic target. Unlabeled cortisone is a glucocorticoid that binds to the glucocorticoid receptor (GR) and mineralocorticoid receptor (MR). Cortisone is an inactive metabolite that is converted to cortisol (active) by 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1). Cortisone-d8 is used solely for analytical quantification.
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| ln Vitro |
Drug compounds have included stable heavy isotopes of carbon, hydrogen, and other elements, mostly as tracers for quantification throughout the drug development process. Due to its potential to alter the pharmacokinetic and metabolic characteristics of medications, deuteration has drawn attention[1].
In vitro, cortisone-d8 has no biological activity as a therapeutic compound. It is used as an internal standard to correct for matrix effects and variations in LC-MS/MS analysis. It is added to biological samples during method development and validation for the accurate measurement of cortisone and other steroid hormones. |
| ln Vivo |
Cortisone-d8 is not administered for therapeutic in vivo activity. It is used as an internal standard in bioanalytical assays for research purposes. When used as a tracer, cortisone-d8 may be administered at very low microdoses to study steroid metabolism, but such studies are uncommon due to its primary role as an analytical reference standard.
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| Enzyme Assay |
For in vitro analytical assays (non-cellular), cortisone-d8 is used as an internal standard in LC-MS/MS. A working solution of cortisone-d8 (e.g., 100 ng/mL in methanol) is prepared. Biological samples (plasma, serum, saliva, urine, 50-200 microL) are spiked with a fixed amount of cortisone-d8. Liquid-liquid extraction (e.g., with methyl tert-butyl ether) or solid-phase extraction (SPE) is performed. The extract is dried, reconstituted, and injected onto an LC-MS/MS system using a C18 column with gradient elution (water/methanol or acetonitrile with 0.1% formic acid). MRM transitions for cortisone-d8 (e.g., m/z 369 → 149 or similar) are monitored. Cortisone-d8 is used for targeted and untargeted metabolomics approaches.
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| Cell Assay |
Cortisone-d8 is not typically used in cell-based assays as a treatment compound. It can be added to cell culture media or cell lysates as a quality control standard or for method validation to quantify endogenous cortisone production or metabolism. Cortisone-d8 is added at a known concentration, and samples are processed and analyzed by LC-MS/MS.
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| Animal Protocol |
Cortisone-d8 is not used in animal efficacy studies as a drug candidate. It may be used as an internal standard for pharmacokinetic studies of cortisone or in tracer studies (minimal quantities). In such studies, a very low microdose (e.g., microg/kg) of cortisone-d8 could be administered to animals (rats or mice) via intravenous or oral routes. Blood is collected at various time points, and plasma is analyzed by LC-MS/MS. However, this is uncommon. Typically, cortisone-d8 is added to blank biological matrices to prepare calibration standards and quality control samples.Cortisone-d8 (CAS: 73546-13-1 or similar; Molecular formula: C21H20D8O5; MW: 368.49 Da) is supplied as a solid (white to off-white powder) or as a 100 microg/mL solution in methanol. Isotopic enrichment: ≥98 atom% D. It is stored at -20degC, protected from light. It is stable for long-term storage under recommended conditions. It is soluble in methanol, ethanol, and DMSO.Cortisone-d8 is a stable isotope-labeled internal standard with minimal toxicity at the trace amounts used (microg/L to mg/L range). Standard laboratory safety practices for handling chemical standards should be followed. Methanol solutions are flammable. Not for human consumption. It is strictly a research reagent for analytical method development (AMV), quality control (QC), and bioanalysis.Cortisone-d8 is used in clinical chemistry and pharmaceutical research for the sensitive and simultaneous measurement of steroid hormones, including cortisol and cortisone, in biological matrices such as serum, plasma, saliva, and urine by LC-MS/MS. It corrects for variability in sample preparation and ionization. It is also used in high-throughput LC/MS metabolomic analysis. It is not approved for human use.
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| References |
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
[2]. Hirano T, et, al. Cortisone counteracts apoptosis-inducing effect of cortisol in human peripheral-blood mononuclear cells. Int Immunopharmacol. 2001 Nov;1(12):2109-15. [3]. McCue RE, et, al. The effect of cortisone on the accumulation, activation, and necrosis of macrophages in tuberculous lesions. Inflammation. 1978 Jun;3(2):159-76. [4]. Seleem D, et, al. In Vivo Antifungal Activity of Monolaurin against Candida albicans Biofilms. Biol Pharm Bull. 2018;41(8):1299-1302. [5]. Rusu VM, et, al. In vivo effects of cortisone on the B cell line in chickens. J Immunol. 1975 Nov;115(5):1370-4. |
| Molecular Formula |
C21H20D8O5
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|---|---|
| Molecular Weight |
368.49
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| Related CAS # |
Cortisone;53-06-5
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7138 mL | 13.5689 mL | 27.1378 mL | |
| 5 mM | 0.5428 mL | 2.7138 mL | 5.4276 mL | |
| 10 mM | 0.2714 mL | 1.3569 mL | 2.7138 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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