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| 250mg |
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| 500mg |
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| 1g |
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Purity: ≥98%
Beclomethasone (also called Beclometasone) is a topically used anti-inflammatory corticosteroid used in treatment of asthma and rhinitis. In addition, Beclomethasone dipropionate has been reported to be previously developed as aqueous nasal formulations for the treatment of Allergic rhinitis. Moreover, Beclomethasone dipropionate has shown the availability in dry nasal aerosol formulations as chiorofluoro carbon metered-dose inhaler nasal sprays.
| 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].
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| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Although not measured, the amounts of inhaled corticosteroids absorbed into the maternal bloodstream and excreted into breastmilk are probably too small to affect a breastfed infant. Expert opinion considers inhaled, nasal and oral corticosteroids acceptable to use during breastfeeding. ◉ Effects in Breastfed Infants None reported with any corticosteroid. Three infants were breastfed for 6 months during maternal treatment with beclomethasone dipropionate by inhaler. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. |
| References | |
| Additional Infomation |
Beclomethasone is a 17alpha-hydroxy steroid that is prednisolone in which the hydrogens at the 9alpha and 16beta positions are substituted by a chlorine and a methyl group, respectively. It has a role as an anti-inflammatory drug and an anti-asthmatic drug. It is an 11beta-hydroxy steroid, a 17alpha-hydroxy steroid, a 20-oxo steroid, a 21-hydroxy steroid, a corticosteroid, a glucocorticoid, a 3-oxo-Delta(1),Delta(4)-steroid, a chlorinated steroid, a primary alpha-hydroxy ketone and a tertiary alpha-hydroxy ketone. It is functionally related to a prednisolone. It derives from a hydride of a 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 immunomodulating properties. After cell surface receptor attachment and cell entry, beclomethasone enters the nucleus where it binds to and activates specific nuclear receptors, resulting in an altered gene expression and inhibition of proinflammatory cytokine production. An anti-inflammatory, synthetic glucocorticoid. It is used topically as an anti-inflammatory agent and in aerosol form for the treatment of ASTHMA. See also: Beclomethasone Dipropionate (active moiety of); Beclomethasone Dipropionate Monohydrate (active moiety of). |
| 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
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| 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
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| 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.
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