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100mg | ||
250mg | ||
500mg |
ln Vitro |
Lung fibroblasts that have been isolated from the lung are inhibited from activating by flunisolide half hydrate (0.1–10 μM, 1 hour) [1]. Flunisolide hemiwater (10 μM, 24 h) causes sputum eosinophil apoptotic death and decreases the release of MMP-9, TIMP-1, TGF-β, and fibronectin from sputum cells isolated from patients with mild to moderate asthma[2]. In BEAS-2B cells, flunisolide hemiwater (0.1–10 µM µM, 24 h) can efficiently block TNF-α-induced ICAM-1 expression as well as GM-CSF and IL-5 production [3]. It has been demonstrated that flunisolide hemihydrate (115 µM, 0–3 hours) is ATP-dependent and can move polarizedly in Calu-3 cells from the apical (ap) to the basolateral (bl) direction [4].
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ln Vivo |
Flunisolide hemihydrate (intranasal treatment, 0.3-10 µg/mouse, daily, days 21-27) can decrease lung inflammation, fibrosis, and airway hyperresponsiveness, and can also alleviate lung inflammation in silicic mice. The removal rate of partial silica particles [1]. Flunisolide hemihydrate (intranasal, 0.3-10 µg/mouse daily, days 21-27) reduces silica-induced accumulation of macrophages and myofibroblasts in lung tissue [ 1].
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Cell Assay |
Apoptosis analysis [2]
Cell Types: eosinophils Tested Concentrations: 10 μM Incubation Duration: 24 h Experimental Results: Induced apoptosis of sputum eosinophils. |
Animal Protocol |
Animal/Disease Models: Male Swiss Webster mouse (intranasal instillation, crystalline silica, 10 mg/50 µL, particle size 0.5-10 µm) [1]
Doses: 0.3-10 µg/mouse daily, p. Results of intranasal administration for 21-27 days: diminished granulomatous reactions, collagen deposition associated with granuloma formation induced by silica particles. Reduce the number of F4/80 and α-SMA positive cells. |
References |
[1]. Tatiana Paula Teixeira Ferreira, et al. Intranasal Flunisolide Suppresses Pathological Alterations Caused by Silica Particles in the Lungs of Mice. Front Endocrinol (Lausanne). 2020 Jun 17;11:388.
[2]. M Profita, et al. In vitro effects of flunisolide on MMP-9, TIMP-1, fibronectin, TGF-beta1 release and apoptosis in sputum cells freshly isolated from mild to moderate asthmatics. Allergy. 2004 Sep;59(9):927-32. [3]. S Boero, et al. Modulation by flunisolide of tumor necrosis factor-alpha-induced stimulation of airway epithelial cell activities related to eosinophil inflammation. J Asthma. 2010 May;47(4):381-7. [4]. B I Florea, et al. Evidence of P-glycoprotein mediated apical to basolateral transport of flunisolide in human broncho-tracheal epithelial cells (Calu-3). Br J Pharmacol. 2001 Dec;134(7):1555-63. |
Molecular Formula |
2[C24H31O6F].H2O
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Molecular Weight |
887.010760000001
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CAS # |
77326-96-6
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Related CAS # |
Flunisolide;3385-03-3;Flunisolide-d6
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SMILES |
O.O=C1C=C[C@@]2(C3[C@@H](O)C[C@@]4([C@@]5(OC(C)(C)O[C@@H]5C[C@H]4[C@@H]3C[C@H](F)C2=C1)C(CO)=O)C)C.O=C1C=C[C@@]2(C3[C@@H](O)C[C@@]4([C@@]5(OC(C)(C)O[C@@H]5C[C@H]4[C@@H]3C[C@H](F)C2=C1)C(CO)=O)C)C
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.1274 mL | 5.6369 mL | 11.2738 mL | |
5 mM | 0.2255 mL | 1.1274 mL | 2.2548 mL | |
10 mM | 0.1127 mL | 0.5637 mL | 1.1274 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.