中文名 | 去异丁基环索奈德 |
英文名 | Desisobutyryl Ciclesonide |
别名 | 环索奈德杂质 环索奈德杂质B 去异丁酰环索奈德 去异丁基环索奈德 去异丁酸酯环索奈德 环索奈德EP杂质B 环索奈德杂质B(EP) 环索奈德杂质B EP标准品 |
英文别名 | CIC-AP Ciclesonide impurity B Desisobutyryl Ciclesonide Ciclesonide EP Impurity B 21-Desisobutyryl Ciclesonide Ciclesonide active principle (11β,16α)-16,17-[[(R)-CyclohexylMethylene]bis(oxy)]-11,21-dihydroxypregna-1,4-diene-3,20-dione |
CAS | 161115-59-9 |
化学式 | C28H38O6 |
分子量 | 470.61 |
密度 | 1.28±0.1 g/cm3(Predicted) |
熔点 | 129-132?C |
沸点 | 640.8±55.0 °C(Predicted) |
溶解度 | 氯仿 (微溶) 、甲醇 (微溶) |
酸度系数 | 12.87±0.10(Predicted) |
存储条件 | -20°C Freezer |
外观 | 整洁 |
颜色 | White to Off-White |
体外研究 | Ciclesonide, an inhaled corticosteroid with almost no affinity for the glucocorticoid receptor, is highly effective in downregulating in vitro pro-inflammatory activities of airway parenchymal cells when converted into the active metabolite Desisobutyryl-ciclesonide. Peripheral blood mononuclear cell proliferation to C. albicans is dose-dependently inhibited by 0.3-3.0 μM Ciclesonide and Desisobutyryl-ciclesonide but inhibition by Desisobutyryl-ciclesonide is higher. A significant proliferation to PhlP5 is observed only in cultures from atopic subjects: an effective downregulation is already detected at 0.03 μM Ciclesonide and 0.003 μM Desisobutyryl-ciclesonide (complete inhibition at 3 μM Ciclesonide and 0.03 μM Desisobutyryl-ciclesonide). 3 μM Ciclesonide and Desisobutyryl-ciclesonide reduce the PhlP5 -specific T-cell blast proliferation and interleukin 4-producing cell proportion. In PBMCs cultures from atopic patients, both Ciclesonide (CIC) and Desisobutyryl-ciclesonide (des-CIC) induce a dose-dependent downregulation of PhlP5 -induced proliferation. The effect is already significantat 0.03 μM Ciclesonide and at 0.003 μM Desisobutyryl-ciclesonide (p<0.001, each comparison),with an early complete inhibition observed at 3μM Ciclesonide and at 0.03 μM Desisobutyryl-ciclesonide. The inhibitory activity toward PhlP5 -induced PBMC proliferation is higher for Desisobutyryl-ciclesonide than for Ciclesonide at 0.003 μM (p<0.05), 0.03 μM (p<0.001) and 0.3 μM (p<0.05). |
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