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| 1mg | ||
| Other Sizes |
| Targets |
The non‑deuterated parent, beclometasone dipropionate, is a potent glucocorticoid receptor agonist. Activation of the glucocorticoid receptor leads to the transcriptional regulation of anti‑inflammatory genes and suppression of pro‑inflammatory mediators, resulting in potent anti‑inflammatory and immunosuppressive activity.
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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].
The non‑deuterated beclometasone dipropionate is an orally active glucocorticoid with potent anti‑inflammatory and immunosuppressive activity. Betamethasone (its active metabolite) appears to be an effective inhibitor of LPS‑induced inflammation and matrix metalloproteinase (MMP) release in vitro. |
| ln Vivo |
Betamethasone dipropionate, the proagent of betamethasone, is an orally active and potent glucocorticoid with anti‑inflammatory and immunosuppressive activity in vivo. Betamethasone inhibits LPS‑induced pulmonary inflammation and reduces MMP activity in bronchoalveolar lavage fluid from exposed mice.
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| Enzyme Assay |
A standard in vitro glucocorticoid receptor binding assay: Human glucocorticoid receptor (GR) protein is incubated with 3H‑dexamethasone (2 nM) and increasing concentrations of test compound (0.1 nM‑10 uM) at 4degC for 16 h. Bound radioactivity is separated by charcoal absorption or filtration, and IC50 values are calculated from competitive binding curves.
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| Cell Assay |
A general cell‑based anti‑inflammatory assay: Human lung epithelial cells (e.g., 16HBE or A549) are seeded in 6‑well plates (1×10⁶ cells/well). Cells are pretreated with beclometasone dipropionate (1 nM‑1 uM) for 1 h, then co‑incubated with 5% cigarette smoke extract (CSE) and IL‑17A (10 ng/mL) for 24 h. Cytokine levels (e.g., IL‑6, IL‑8) in the supernatant are measured by ELISA.
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| Animal Protocol |
A general animal model of inflammation: Balb/c mice are exposed to aerosolised LPS (0.5 mg/mL) for 30 min to induce pulmonary inflammation. Beclometasone dipropionate (1‑10 mg/kg) is administered orally or intranasally 1 h before LPS challenge. After 6 h, bronchoalveolar lavage fluid (BALF) is collected for differential cell count and MMP activity measurement.
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| ADME/Pharmacokinetics |
As a stable isotope‑labeled compound, beclometasone dipropionate‑d10 is expected to have PK properties similar to the non‑deuterated form. It is used as an internal standard in LC‑MS/MS to quantify the parent drug in biological matrices. The unlabeled compound is rapidly absorbed and extensively metabolised to its active metabolite betamethasone, with a plasma half‑life of approximately 2‑3 h.
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| Toxicity/Toxicokinetics |
The non‑deuterated beclometasone dipropionate has an LD50 > 4000 mg/kg in rats (oral). Long‑term use in humans can cause adrenal suppression, osteoporosis and increased infection risk. As a research‑grade isotopologue, similar toxicity is expected, but full toxicological studies are not available for the deuterated form.
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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]. Paola Lovato, et al. Calcipotriol and betamethasone dipropionate exert additive inhibitory effects on the cytokine expression of inflammatory dendritic cell-Th17 cell axis in psoriasis. J Dermatol Sci. 2016 Mar;81(3):153-64. [3]. M Corbel, et al. Comparative effects of betamethasone, cyclosporin and nedocromil sodium in acute pulmonary inflammation and metalloproteinase activities in bronchoalveolar lavage fluid from mice exposed to lipopolysaccharide. Pulm Pharmacol Ther. 1999;12(3):165-71. |
| Additional Infomation |
Beclometasone dipropionate is widely used clinically for asthma (via inhalation) and allergic rhinitis (via intranasal spray). The deuterated version is for research use only and serves as an internal standard for bioanalysis, enabling accurate quantitation in pharmacokinetic studies. It is not intended for therapeutic use.
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| Molecular Formula |
C28H27D10CLO7
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| Molecular Weight |
531.10
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| Related CAS # |
Beclometasone dipropionate;5534-09-8
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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 | 1.8829 mL | 9.4144 mL | 18.8288 mL | |
| 5 mM | 0.3766 mL | 1.8829 mL | 3.7658 mL | |
| 10 mM | 0.1883 mL | 0.9414 mL | 1.8829 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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