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| 1mg | ||
| Other Sizes |
| Targets |
Betamethasone-d5 targets the glucocorticoid receptor (GR), an intracellular protein that, upon ligand binding, translocates to the nucleus to modulate gene expression. As a synthetic glucocorticoid, betamethasone binds to the GR with high affinity, leading to both transactivation and transrepression of target genes. This results in broad anti-inflammatory effects, suppression of immune responses, and acceleration of fetal lung maturation. The deuterated version retains the same receptor binding affinity and pharmacological activity as the non-labeled compound.
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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].
Betamethasone, the parent compound, exerts its effects by binding to the glucocorticoid receptor, leading to the activation of anti-inflammatory genes and repression of pro-inflammatory transcription factors such as NF-kappaB and AP-1. In vitro, betamethasone induces apoptosis in various cell types and stimulates gene expression changes that promote lung epithelial cell differentiation. Specific EC50 values for betamethasone-d5 are not detailed, as it is primarily used as an analytical standard rather than in functional assays. |
| ln Vivo |
Betamethasone-d5 is not typically used in in vivo functional studies, as it is an analytical standard for quantifying betamethasone levels. However, the parent compound betamethasone has well-established in vivo pharmacological activities, including anti-inflammatory, immunosuppressive, and fetal lung maturation effects. Betamethasone is clinically used in pregnant women to accelerate fetal lung maturation and in various inflammatory and autoimmune conditions. As an analytical standard, betamethasone-d5 is used in animal pharmacokinetic studies to trace betamethasone distribution and metabolism.
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| Enzyme Assay |
Binding studies for betamethasone-d5 are typically performed using the same methods as for non-labeled betamethasone. These involve competitive radioligand binding assays using the glucocorticoid receptor. The compound is incubated with cell lysates or purified GR protein in the presence of a radiolabeled glucocorticoid such as 3H-dexamethasone. After incubation and separation of bound and free ligand, radioactivity is measured. The deuterated form is used as a competitor to determine binding affinity and specificity.
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| Cell Assay |
In vitro cellular experiments for betamethasone-d5 are not typically performed because it is an analytical standard. However, the parent compound betamethasone is used in cell-based assays to study glucocorticoid receptor activation. Cells expressing GR (e.g., A549 lung epithelial cells, HeLa, or primary lymphocytes) are treated with various concentrations of betamethasone. Endpoints include measurement of GR translocation by immunofluorescence, quantification of GR target gene expression (e.g., GILZ, MKP-1, IL-10) by RT-PCR or ELISA, and assessment of anti-inflammatory effects (e.g., inhibition of TNF-alpha or IL-6 production in stimulated cells).
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| Animal Protocol |
In vivo animal protocols for betamethasone-d5 are typically part of pharmacokinetic or metabolism studies. The compound is administered to rodents (e.g., rats or mice) by intravenous, intramuscular, or oral administration at specified doses (e.g., 1-10 mg/kg). Blood samples are collected at various time points post-dose (e.g., 0, 15, 30, 60, 120, 240, 480 minutes). Plasma concentrations of betamethasone-d5 are measured by LC-MS/MS, and the deuterated standard is used for calibration and quantification of unlabeled betamethasone in the same samples. Tissue distribution studies may also be performed.
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| ADME/Pharmacokinetics |
Betamethasone-d5 is used as an internal standard for the quantification of betamethasone in pharmacokinetic studies. Its deuterium substitution (5 deuterium atoms) results in a mass shift that allows it to be distinguished from the unlabeled compound by mass spectrometry while maintaining virtually identical chemical and physical properties. This improves the accuracy and precision of drug concentration measurements in biological samples. The deuterated form is stable and does not undergo deuterium-hydrogen exchange under typical analytical conditions.
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| Toxicity/Toxicokinetics |
Toxicological data for betamethasone-d5 are not extensively reported, as it is an analytical standard and research tool. The parent compound betamethasone, as a potent glucocorticoid, is known to cause numerous side effects with chronic or high-dose use, including hyperglycemia, immunosuppression, osteoporosis, adrenal suppression, growth retardation, and Cushing's syndrome. However, as a stable isotope-labeled compound used at very low concentrations in analytical applications, betamethasone-d5 does not pose significant toxicological risks beyond those of the unlabeled compound. Standard laboratory chemical safety precautions apply.
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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]. Schwab M, et, al. Effects of betamethasone administration to the fetal sheep in late gestation on fetal cerebral blood flow. J Physiol. 2000 Nov 1;528(Pt 3):619-32. [3]. Xie W, et, al. Betamethasone affects cerebral expressions of NF-kappaB and cytokines that correlate with pain behavior in a rat model of neuropathy. Ann Clin Lab Sci. Winter 2006;36(1):39-46. [4]. Kubin ME, et, al. Clinical Efficiency of Topical Calcipotriol/Betamethasone Treatment in Psoriasis Relies on Suppression of the Inflammatory TNFα - IL-23 - IL-17 Axis. Acta Derm Venereol. 2017 Apr 6;97(4):449-455. [5]. Hofmann TH, et, al. Various glucocorticoids differ in their ability to induce gene expression, apoptosis and to repress NF-kappaB-dependent transcription. FEBS Lett. 1998 Dec 28;441(3):441-6. |
| Additional Infomation |
Betamethasone-d5 has the molecular formula C22H24D5FO5 and a molecular weight of 397.49. The unlabeled betamethasone has a CAS number of 378-44-9. The deuterated form is used as an internal standard for the quantification of betamethasone in biological samples by LC-MS/MS. Betamethasone is a synthetic glucocorticoid with potent anti-inflammatory and immunosuppressive activities, clinically used for various inflammatory and autoimmune conditions and to accelerate fetal lung maturation. The product is for research use only and is not for human therapeutic use.
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| Molecular Formula |
C22H24D5FO5
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|---|---|
| Molecular Weight |
397.49
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| Related CAS # |
Betamethasone;378-44-9
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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 | 2.5158 mL | 12.5789 mL | 25.1579 mL | |
| 5 mM | 0.5032 mL | 2.5158 mL | 5.0316 mL | |
| 10 mM | 0.2516 mL | 1.2579 mL | 2.5158 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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