Flunisolide

Research use only, not for human use.

Flunisolide (marketed as AeroBid, Nasalide, Nasarel) is a corticosteroid often prescribed as treatment for allergic rhinitis.

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.

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.

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.

RS 3999

Endocrinology/Hormones

GR

Glucocorticoid Receptor

Inflammation/Immunology

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3385-03-3

434.5

C24H31FO6

>98% (HPLC)

DMSO: 10 mM

O=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

(1S,2S,4R,8S,9S,11S,12S,13R,19S)-19-fluoro-11-hydroxy-8-(2-hydroxyacetyl)-6,6,9,13-tetramethyl-5,7-dioxapentacyclo[10.8.0.02,9.04,8.013,18]icosa-14,17-dien-16-one

(-20℃)

With Ice Pack

≥ 2 years