Desisobutyryl Ciclesonide

糖皮质激素受体激动剂和环索奈德的活性代谢物；与糖皮质激素受体结合(IC50=1.75nM)；抑制刀豆球蛋白A诱导的原代大鼠脾细胞和人类PBMCs增殖(IC50s分别为1.5和1.3nM)；抑制CD3诱导的人类CD4+淋巴细胞增殖(IC50=0.2nM)和相同细胞中细胞因子的产生(IC50s=0.5-1.5nM)；减少用卵清蛋白致敏和刺激的大鼠BALF中的嗜酸性粒细胞、TNF-α和总蛋白积累(ED50s分别为0.7、0.4和0.5mg/kg)。A glucocorticoid receptor agonist and the active metabolite of ciclesonide; binds to the glucocorticoid receptor (IC50 = 1.75 nM); inhibits concanavalin A-induced proliferation of primary rat spleen cells and human PBMCs (IC50s = 1.5 and 1.3 nM, respectively); 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); reduces eosinophil, TNF-α, and total protein accumulation in the BALF of rats sensitized and challenged with ovalbumin (ED50s = 0.7, 0.4, and 0.5 mg/kg, respectively).分子式C28H38O6分子量470.6C[C@@]12[C@@]3(C(CO)=O)[C@@](O[C@](C4CCCCC4)([H])O3)([H])C[C@@]1([H])[C@@]5([H])[C@]([C@@]6(C(CC5)=CC(C=C6)=O)C)([H])[C@H](C2)O