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Ciclesonide (Synonyms: CIC, RPR 251526)

رقم الكتالوجGC17571 Copy One-Click Copy Product Info

Ciclesonide (RPR251526) هو جلايكورتيكويد مع نشاط قوي مضاد للالتهابات

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Ciclesonide التركيب الكيميائي

Cas No.: 126544-47-6

الحجم السعر المخزون الكميّة
10mM (in 1mL DMSO)
38٫00
متوفر
5mg
22٫00
متوفر
10mg
35٫00
متوفر
50mg
101٫00
متوفر
100mg
164٫00
متوفر

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مراجعات العميل

بناء على آراء العملاء.

Sample solution is provided at 25 µL, 10mM.



Description of Ciclesonide

Ciclesonide(RPR251526) is a glucocorticoid used to treat obstructive airway diseases.Target: Glucocorticoid ReceptorCiclesonide (CIC) is an inhaled glucocorticosteroid. CIC (5 microM) was rapidly hydrolyzed by NHBE cells (approximately 30% conversion at 4h), with almost complete conversion by 24h. In liver and NHBE cells, major involvement of cytosolic carboxylesterases, with some contribution by cholinesterases, was indicated. The highest level of conversion was found in the liver, the site of inactivation of des-CIC through rapid oxidation by cytochrome P450. Carboxylesterases in bronchial epithelial cells probably contribute significantly to the conversion to des-CIC in the target organ, whereas low systemic levels of des-CIC are a result of the high metabolic clearance by the liver following CIC inhalation [1]. Ciclesonide may have some advantage although it is not as yet licensed in all countries for paediatric use [2].

References:
[1]. Mutch, E., et al., The role of esterases in the metabolism of ciclesonide to desisobutyryl-ciclesonide in human tissue. Biochem Pharmacol, 2007. 73(10): p. 1657-64.
[2]. Barnes, N.C., The properties of inhaled corticosteroids: similarities and differences. Prim Care Respir J, 2007. 16(3): p. 149-54.

Protocol of Ciclesonide

Cell experiment:

Peripheral blood mononuclear cells are isolated from non atopic and atopic asthmatic children sensitized to Phleum pratense (PhlP5). Proliferation toward Candida albicans or PhlP5 in the presence of Ciclesonide or Desisobutyryl-ciclesonide (0.003-3.0 μM) is evaluated as [3H]thymidine incorporation. Modulation of PhlP5-specific T-cell blasts proliferation and PhlP5-induced interleukin 4 expression by Ciclesonide and Desisobutyryl-ciclesonide are measured[1].

References:

[1]. Silvestri M, et al. Ciclesonide modulates in vitro allergen-driven activation of blood mononuclear cells and allergen-specific T-cell blasts. Immunol Lett. 2012 Jan 30;141(2):190-6.

Chemical Properties of Ciclesonide

Cas No. 126544-47-6 SDF
المرادفات CIC, RPR 251526
Chemical Name 2-((6aR,6bS,7S,8aS,8bS,10R,11aR,12aS,12bS)-10-cyclohexyl-7-hydroxy-6a,8a-dimethyl-4-oxo-2,4,6a,6b,7,8,8a,8b,11a,12,12a,12b-dodecahydro-1H-naphtho[2',1':4,5]indeno[1,2-d][1,3]dioxol-8b-yl)-2-oxoethyl isobutyrate
Canonical SMILES CC(C(OCC([C@@]12[C@@](O[C@@](O2)([H])C3CCCCC3)([H])C[C@@]4([H])[C@]([C@]5([H])[C@](O)([H])C[C@@]41C)([H])CCC6=CC(C=C[C@@]65C)=O)=O)=O)C
Formula C32H44O7 M.Wt 540.69
الذوبان ≥ 15.8mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Ciclesonide

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 1.8495 mL 9.2474 mL 18.4949 mL
5 mM 369.9 μL 1.8495 mL 3.699 mL
10 mM 184.9 μL 924.7 μL 1.8495 mL
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In vivo Formulation Calculator (Clear solution) of Ciclesonide

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 20 reference(s) in Google Scholar.)

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