Formulation: A solid
Formal Name: 16α,17-[[(R)-cyclohexylmethylene]bis(oxy)]-11β,21-dihydroxy-pregna-1,4-diene-3,20-dione
Purity: ≥95%
Formula Markup: C28H38O6
Formula Weight: 470,6
Shelf life (days): 1460
CAS Number: 161115-59-9
Notes: Desisobutyryl ciclesonide is a glucocorticoid receptor agonist and the active metabolite of the prodrug ciclesonide (Item No. 18227).{29502,58699} It is formed from inhaled ciclesonide by intracellular esterases in the lung. Desisobutyryl ciclesonide binds to the glucocorticoid receptor (IC50 = 1.75 nM for the human receptor) and induces glucocorticoid receptor-mediated gene transactivation in a reporter assay. It inhibits concanavalin A-induced proliferation of primary rat spleen cells and human peripheral blood mononuclear cells (PBMCs; IC50s = 1.5 and 1.3 nM, respectively). Desisobutyryl ciclesonide also inhibits CD3-induced proliferation of human CD4+ lymphocytes (IC50 = 0.2 nM) and the production of cytokines in the same cells (IC50s = 0.5-1.5 nM).{58700} It reduces eosinophil, TNF-α, and total protein accumulation in bronchoalveolar lavage fluid (BALF) of rats sensitized and challenged with ovalbumin (ED50s = 0.7, 0.4, and 0.5 mg/kg, respectively).
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