Catalogue Number: B3477-APE
|Physical state:||A solid|
|Shipping Condition:||Blue Ice|
|Unit(s):||10 mg, 50 mg|
Description: 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.
Store at -20°C
insoluble in H2O; ≥15.8 mg/mL in DMSO; ≥50.6 mg/mL in EtOH