Ciclesonide

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Ciclesonide

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

126544-47-6

包装与价格：

包装	价格(元)
10mg	电议
50mg	电议

产品介绍

化学性质

Physical Appearance	A solid
Storage	Store at -20°C
M.Wt	540.69
Cas No.	126544-47-6
Formula	C₃₂H₄₄O₇
Solubility	insoluble in H2O; ≥15.8 mg/mL in DMSO; ≥50.6 mg/mL in EtOH
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
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

Ciclesonide is a prodrug of the potent glucocorticoid receptor agonist desisobutyryl-ciclesonide. Ciclesonide undergoes the hydrolysis process by ester cleavage at the C21 position to desisobutyryl-ciclesonide, followed by reversible formation of fatty acid esters in lung cells. Although both ciclesonide and desisobutyryl-ciclesonide are able to bind to the glucocorticoid receptor, the active metabolite desisobutyryl-ciclesonide (IC50 = 210 nM) is about 100-fold more potent than the parent compound ciclesonide (IC50 = 1.75 nM). Formulations containing ciclesonide have been used in the maintenance treatment of asthma and in the treatment of allergic rhinitis.

References:

1. Derendorf H, Nave R, Drollmann A, et al. Relevance of pharmacokinetics and pharmacodynamics of inhaled corticosteroids to asthma. European Respiratory Journal, 2006, 28(5): 1042-1050.

2. Mutch E, Nave R, McCracken N, et al. The role of esterases in the metabolism of ciclesonide to desisobutyryl-ciclesonide in human tissue. Biochemical Pharmacology, 2007, 73(10): 1657-1664.

3. Belvisi MG, Bundschuh DS, Stoeck M, et al. Preclinical profile of ciclesonide, a novel corticosteroid for the treatment of asthma. Journal of Pharmacology and Experimental Therapeutics, 2005, 314(2): 568-574.

试验操作

Cell experiment:[2]
Cell lines	Normal human bronchial epithelial (NHBE) cells
Reaction Conditions	5 μM ciclesonide for 24 h incubation
Applications	Ciclesonide (5 μM) was rapidly hydrolyzed to desisobutyryl-ciclesonide by NHBE cells (approximately 30% conversion within the first 4 h), and 96% conversion of ciclesonide to desisobutyryl-ciclesonide was achieved at 24 h.
Animal experiment:[3]
Animal models	Ovalbumin-sensitized and challenged Brown Norway rats
Dosage form	0 ~ 10 mg/kg Administered by the intratracheal route into the airways 24 and 1 h before exposure to inhaled antigen
Applications	Ciclesonide dose-dependently suppressed the antigen-induced influx of eosinophils into the airway lumen, with an ED50 value of 0.75 mg/kg. Moreover, ciclesonide significantly inhibited eosinophil influx into the lung tissue, with an ED50 value of 0.49 mg/kg.
Note	The technical data provided above is for reference only.
	References: 1. Derendorf H, Nave R, Drollmann A, et al. Relevance of pharmacokinetics and pharmacodynamics of inhaled corticosteroids to asthma. European Respiratory Journal, 2006, 28(5): 1042-1050. 2. Mutch E, Nave R, McCracken N, et al. The role of esterases in the metabolism of ciclesonide to desisobutyryl-ciclesonide in human tissue. Biochemical Pharmacology, 2007, 73(10): 1657-1664. 3. Belvisi MG, Bundschuh DS, Stoeck M, et al. Preclinical profile of ciclesonide, a novel corticosteroid for the treatment of asthma. Journal of Pharmacology and Experimental Therapeutics, 2005, 314(2): 568-574.