| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
Budesonide-d8 targets the glucocorticoid receptor (GR), a nuclear receptor that regulates gene transcription in response to glucocorticoids. Budesonide is a potent glucocorticoid receptor agonist with an EC50 of 45.7 pM in a transactivation assay. It is selective for glucocorticoid over mineralocorticoid receptors (EC50 = 7,620 pM). As a deuterated internal standard, Budesonide-d8 does not exert pharmacological activity in assays but serves as a reference for quantification.
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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 effect on a drug's pharmacokinetics and metabolic properties, it is a cause for concern [1].
In vitro, Budesonide-d8 is used as an internal standard for the quantification of budesonide in biological samples. Budesonide itself is a potent anti-inflammatory agent that acts by inhibiting the production of pro-inflammatory cytokines and chemokines. Budesonide-d8 has the same chemical properties as budesonide but with a different mass due to deuterium substitution, allowing for accurate quantification by mass spectrometry. |
| ln Vivo |
In vivo, Budesonide-d8 is used as an internal standard in pharmacokinetic studies to accurately measure budesonide concentrations. Budesonide is an inhaled glucocorticoid used in the treatment of various inflammatory conditions, including asthma and inflammatory bowel disease. It is an orally active glucocorticoid receptor agonist that reduces lung tumor volume. Budesonide-d8 is not administered as a therapeutic agent.
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| Enzyme Assay |
For in vitro analytical assays, Budesonide-d8 is spiked into biological samples (such as plasma, urine, or tissue homogenates) at known concentrations. Samples are extracted and analyzed by LC-MS or GC-MS. The ratio of Budesonide-d8 to budesonide is used to calculate the concentration of budesonide in the sample.
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| Cell Assay |
For cell-based assays, Budesonide-d8 is not typically used for biological activity studies. Instead, it is used as an internal standard in LC-MS analysis of cell lysates or culture media from cells treated with budesonide. The compound's deuterated nature allows for accurate quantification of budesonide uptake, metabolism, and cellular responses.
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| Animal Protocol |
For in vivo pharmacokinetic studies, Budesonide-d8 is administered to animals alongside budesonide or as a separate dose. Blood samples are collected at various time points, and plasma is analyzed by LC-MS using Budesonide-d8 as the internal standard. Pharmacokinetic parameters such as half-life, Cmax, AUC, and clearance are calculated.
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| ADME/Pharmacokinetics |
Budesonide-d8 has a molecular weight of 438.58 and contains eight deuterium atoms. It is soluble in organic solvents. Storage is recommended at -20°C for long-term stability. The compound is for research use only and is not intended for human or veterinary use.
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| Toxicity/Toxicokinetics |
Toxicological data for Budesonide-d8 are not separately reported, as it is a deuterated internal standard used at trace concentrations. Budesonide itself is well-tolerated at therapeutic doses, with common adverse effects including local irritation and immunosuppression. As a research compound, standard safety precautions should be followed.
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| References |
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| Additional Infomation |
Budesonide-d8 is a deuterated form of budesonide featuring eight deuterium atoms, used as an internal standard for the quantification of budesonide by GC- or LC-MS. Budesonide is a potent glucocorticoid receptor agonist with an EC50 of 45.7 pM. Budesonide-d8 is a research tool for analytical and pharmacokinetic studies and is not approved for clinical use.
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| Molecular Formula |
C25H34O6
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|---|---|
| Molecular Weight |
438.583161830902
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| Exact Mass |
438.286
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| CAS # |
1105542-94-6
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| Related CAS # |
Budesonide;51333-22-3
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| PubChem CID |
12796588
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| Appearance |
White to off-white solid powder
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| LogP |
2.716
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
31
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| Complexity |
862
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| Defined Atom Stereocenter Count |
8
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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 | 2.2801 mL | 11.4004 mL | 22.8009 mL | |
| 5 mM | 0.4560 mL | 2.2801 mL | 4.5602 mL | |
| 10 mM | 0.2280 mL | 1.1400 mL | 2.2801 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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