Flunisolide hemihydrate 是一种皮质类固醇,是具有口服活性的糖皮质激素受体 (Glucocorticoid Receptor) 激活剂,具有抗炎活性。Flunisolide hemihydrate 可诱导嗜酸性粒细胞凋亡 (Apoptosis),可用于哮喘或鼻炎、炎症的相关研究。
产品描述
Flunisolide hemihydrate is a corticosteroid, which is an orally active glucocorticoid receptor activator with anti-inflammatory activity. Flunisolide hemihydrate can induce eosinophil apoptosis, and is used for the research of asthma or rhinitis, and inflammation [1] [2].
体外活性
Flunisolide hemihydrate (0.1-10 μM, 1 h) inhibits lung fibroblast (Isolated from lung) activation [1]. Flunisolide hemihydrate (10 μM, 24 h) reduces MMP-9, TIMP-1, TGF-β and fibronectin release by sputum cells (isolated from mild to moderate asthmatics), and induces sputum eosinophil apoptosis [2]. Flunisolide hemihydrate (0.1-10 μM μM, 24 h) effectively inhibits ICAM-1 expression and GM-CSF and IL-5 release induced by TNF-alpha in BEAS-2B cells [3]. Flunisolide hemihydrate (115 μM, 0-3 h) can be transported in a polarized way in the apical (ap) to basolateral (bl) direction in Calu-3 cells and is demonstrated to be ATP-dependent [4]. Apoptosis Analysis [2] Cell Line: Eosinophil Concentration: 10 μM Incubation Time: 24 h Result: Induced sputum eosinophil apoptosis.
体内活性
Flunisolide hemihydrate (Intranasal administration, 0.3-10 μg/mouse, daily, from days 21–27) inhibits lung inflammation, fibrosis, and airway hyper-reactivity, also improves clearance of silica particles from the lungs in silicotic mice [1]. Flunisolide hemihydrate (Intranasal administration, 0.3-10 μg/mouse, daily, from days 21–27) inhibits silica-induced macrophage and myofibroblast accumulation in the lung tissue [1]. Animal Model: Male Swiss Webster mice (instilled, intranasally, with crystalline silica, 10 mg/50 μL, particle size 0.5-10 μm) [1] Dosage: 0.3-10 μg/mouse, daily, from days 21–27 Administration: Intranasal administration Result: Reduced both granulomatous response, collagen deposition, concerning granuloma formation caused by silica particles. Reduced the number of F4/80 and α-SMA positive cells.
Cas No.
77326-96-6
分子式
C24H31FO6.1/2H2O
分子量
443.51
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years