| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg | |||
| 500mg | |||
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| Other Sizes |
Purity: ≥98%
| Targets |
Beclometasone acts as a glucocorticoid receptor agonist. It binds to the glucocorticoid receptor in the cytoplasm, leading to the translocation of the receptor complex into the nucleus. There, it modulates gene transcription, resulting in the upregulation of anti-inflammatory proteins (such as lipocortin-1) and the downregulation of pro-inflammatory cytokines, chemokines, and adhesion molecules.
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| ln Vitro |
Four hours after the administration of 25 micrograms of beclomethasone, there was inhibition of both injury-induced inflammation-guided neutrophil chemotaxis and normal physiological neutrophil migration. Moreover, incubating embryos in 25 μM beclomethasone four hours before to implantation decreased tumor cell invasion and micrometastases. Furthermore, β-aminopropionitrile (βAPN), a lysyl oxidase inhibitor, has the ability to dramatically lower fibrillar collagen and accelerate neutrophil CHT-TF movement, which in turn increases tumor cell invasion and the subsequent development of micrometastases. Interestingly, βAPN prevents neutrophil chemotaxis generated by inflammation, suggesting that greater non-pathological neutrophil migration but not inflammation is linked to higher tumor cell invasion in βAPN-treated embryos [1].
In vitro, beclometasone exhibits potent anti-inflammatory activity. It inhibits the release of inflammatory mediators from various cell types, including macrophages, mast cells, and lymphocytes. It reduces the production of pro-inflammatory cytokines such as IL-1, IL-6, and TNF-α. It also suppresses the proliferation of T-lymphocytes and inhibits the expression of adhesion molecules on endothelial cells. |
| ln Vivo |
In vivo, beclometasone is used primarily as an inhaled corticosteroid for the management of asthma and chronic obstructive pulmonary disease (COPD). It is also used topically to treat eczema, psoriasis, and other inflammatory skin conditions, and intranasally for allergic rhinitis. It reduces airway inflammation, hyperresponsiveness, and mucus production in the lungs.
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| Enzyme Assay |
The in vitro receptor binding assay for beclometasone involves measuring its affinity for the glucocorticoid receptor. This is typically done using a radioligand binding assay with [³H]-dexamethasone and cytosol preparations from tissues rich in glucocorticoid receptors. The concentration of beclometasone required to displace 50% of the bound radiolabeled ligand (IC50) is determined.
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| Cell Assay |
In vitro cellular assays for beclometasone involve measuring its anti-inflammatory effects on cultured cells. For example, lipopolysaccharide (LPS)-stimulated macrophages are treated with beclometasone, and the production of pro-inflammatory cytokines (e.g., TNF-α, IL-6) in the supernatant is measured by ELISA. The IC50 for cytokine inhibition is determined to assess its potency.
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| Animal Protocol |
In vivo animal experiments for beclometasone are often conducted using models of airway inflammation, such as the ovalbumin-induced asthma model in mice or rats. Animals are sensitized and challenged with ovalbumin to induce airway inflammation. Beclometasone is administered (e.g., intratracheally or by inhalation), and parameters such as airway hyperresponsiveness, inflammatory cell infiltration in bronchoalveolar lavage fluid (BALF), and cytokine levels are measured.
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| ADME/Pharmacokinetics |
Beclometasone is rapidly absorbed after inhalation, and the prodrug is hydrolyzed to its active metabolite, beclomethasone-17-monopropionate (BMP), in the lungs. BMP has a high systemic clearance, which limits its systemic bioavailability. The plasma half-life of beclometasone is very short (approximately 0.5 hours), while BMP has a half-life of about 2.7 hours. The drug is primarily metabolized in the liver by CYP3A4 and excreted in the feces.
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| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Lactation Use Although measurements were not performed, the amount of inhaled corticosteroids absorbed into the mother's bloodstream and secreted into breast milk is likely too small to affect breastfed infants. Expert opinion is that inhaled, nasal, and oral corticosteroids are safe to use during lactation. ◉ Effects on Breastfed Infants No effects on breastfed infants have been reported with any corticosteroids. Three infants were breastfed for 6 months while their mothers were treated with inhaled beclomethasone. ◉ Effects on Lactation and Breast Milk As of the revision date, no relevant published information was found. Beclometasone is generally well-tolerated when used at recommended doses. Common local side effects include hoarseness, throat irritation, and oral candidiasis (thrush). Systemic side effects are rare with inhaled use but can include adrenal suppression, growth retardation in children, and osteoporosis with long-term, high-dose use. It should be used with caution in patients with active tuberculosis or systemic infections. |
| References | |
| Additional Infomation |
Beclomethasone is a 17α-hydroxysteroid, a structural derivative of prednisolone, with its 9α and 16β hydrogen atoms replaced by chlorine and methyl atoms, respectively. It possesses anti-inflammatory and anti-asthmatic effects. Beclomethasone is a 11β-hydroxysteroid, 17α-hydroxysteroid, 20-oxosteroid, 21-hydroxysteroid, corticosteroid, glucocorticoid, 3-oxo-Δ1,Δ4-steroid, chlorinated steroid, primary α-hydroxy ketone, and tertiary α-hydroxy ketone. Functionally, it is related to prednisolone. It is derived from the hydride of pregnane. Beclomethasone is a corticosteroid. The mechanism of action of beclomethasone is as a corticosteroid hormone receptor agonist. Beclomethasone is a synthetic glucocorticoid with anti-inflammatory and immunomodulatory properties. Beclomethasone binds to cell surface receptors and enters the cell, then into the nucleus, where it binds to and activates specific nuclear receptors, thereby altering gene expression and inhibiting the production of pro-inflammatory cytokines. It is an anti-inflammatory synthetic glucocorticoid. It can be used topically as an anti-inflammatory drug and can also be inhaled via nebulizer to treat asthma. See also: Beclomethasone dipropionate (active ingredient); Beclomethasone dipropionate monohydrate (active ingredient).
Beclometasone is marketed under various brand names, including Qvar, Beclovent, and Vanceril. It was first approved for medical use in the 1970s and is on the World Health Organization's List of Essential Medicines. It is available in various formulations, including metered-dose inhalers, dry powder inhalers, nasal sprays, and topical creams and ointments. Its effectiveness in reducing airway inflammation has made it a cornerstone in the treatment of asthma. |
| Molecular Formula |
C22H29CLO5
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|---|---|
| Molecular Weight |
408.919
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| Exact Mass |
520.222
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| CAS # |
4419-39-0
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| Related CAS # |
Beclometasone dipropionate;5534-09-8;Beclomethasone-d5;1263143-48-1
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| PubChem CID |
20469
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
630.5±55.0 °C at 760 mmHg
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| Melting Point |
210ºC
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| Flash Point |
335.1±31.5 °C
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| Vapour Pressure |
0.0±4.2 mmHg at 25°C
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| Index of Refraction |
1.564
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| LogP |
4.59
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
28
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| Complexity |
805
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| Defined Atom Stereocenter Count |
8
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| SMILES |
C[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@@]4([C@]3([C@H](C[C@@]2([C@]1(C(=O)CO)O)C)O)Cl)C
|
| InChi Key |
NBMKJKDGKREAPL-DVTGEIKXSA-N
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| InChi Code |
InChI=1S/C22H29ClO5/c1-12-8-16-15-5-4-13-9-14(25)6-7-19(13,2)21(15,23)17(26)10-20(16,3)22(12,28)18(27)11-24/h6-7,9,12,15-17,24,26,28H,4-5,8,10-11H2,1-3H3/t12-,15-,16-,17-,19-,20-,21-,22-/m0/s1 SMILES
|
| Chemical Name |
9-Chloro-11beta,17,21-trihydroxy-16beta-methylpregna-1,4-diene-3,20-dione
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| Synonyms |
Beclometasone Beclomethasone
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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) |
DMSO : ≥ 32 mg/mL (~78.25 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.25 mg/mL (5.50 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 22.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.25 mg/mL (5.50 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 22.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.25 mg/mL (5.50 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4455 mL | 12.2273 mL | 24.4547 mL | |
| 5 mM | 0.4891 mL | 2.4455 mL | 4.8909 mL | |
| 10 mM | 0.2445 mL | 1.2227 mL | 2.4455 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.
The Effects of Beclomethasone Upper the Endotracheal Cuff on the Occurrence of Sore Throat at Extubation
CTID: NCT02687100
Phase: Phase 4 Status: Withdr
Efficacy of nebulised beclometasone versus placebo in preventing viral wheezing in pre-school children
CTID: null
Phase: Phase 4 Status: Completed
Date: 2009-10-04
Products are for research use only; We do not sell to patients
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