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Flunisolide

SKU: orb1225262

Description

Flunisolide (marketed as AeroBid, Nasalide, Nasarel) is a corticosteroid often prescribed as treatment for allergic rhinitis. The principle mechanism of action of flunisolide is to activate glucocorticoid receptors. It also has anti-inflammatory action.(In Vitro):Flunisolide (0.1-10 μM, 1 h) inhibits lung fibroblast (Isolated from lung) activation.Flunisolide (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.Flunisolide (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.Flunisolide (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.(In Vivo):Flunisolide (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.Flunisolide (Intranasal administration, 0.3–10 μg/mouse, daily, from days 21-27) inhibits silica-induced macrophage and myofibroblast accumulation in the lung tissue.

Images & Validation

Key Properties

CAS Number3385-03-3
MW434.5
Purity>98% (HPLC)
FormulaC24H31FO6
SMILESO=C1C=C[C@]2(C)[C@@]3([H])[C@@H](O)C[C@]4(C)[C@]5(C(CO)=O)OC(C)(C)O[C@]5([H])C[C@@]4([H])[C@]3([H])C[C@H](F)C2=C1
TargetGR
SolubilityDMSO: 10 mM

Bioactivity

In Vivo
Flunisolide (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. Flunisolide (Intranasal administration, 0.3–10 μg/mouse, daily, from days 21-27) inhibits silica-induced macrophage and myofibroblast accumulation in the lung tissue. Animal model: Male Swiss Webster mice (instilled, intranasally, with crystalline silica, 10 mg/50 μL, particle size 0.5-10 μm). 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.
In Vitro
Flunisolide (0.1-10 μM, 1 h) inhibits lung fibroblast (Isolated from lung) activation. Flunisolide (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. Flunisolide (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. Flunisolide (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. Apoptosis Analysis Cell line: Eosinophil. Concentration: 10 μM. Incubation time: 24 h. Result: Induced sputum eosinophil apoptosis.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

RS 3999

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Flunisolide (orb1225262)

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