| Size | Price | |
|---|---|---|
| 25mg | ||
| 50mg | ||
| 100mg | ||
| 250mg |
Fluticasone dipropionate (Cutivate) is an inhaled corticosteroid used for the treatment of respiratory diseases such as itching, dryness, scaling, inflammation, and redness associated with skin conditions like allergic reactions, eczema, and insect or bug bites.
| Targets |
Corticosteroid; SMO
|
|---|---|
| ln Vitro |
Fluticasone (10-1000 nM, 48 hours) decreases HRV-induced mucin formation and is involved in the regulation of SPDEF regulatory genes and extracellular ATP release [3]. Fluticasone (0-10 μM, 2 hours) suppresses the proliferation of U2OS cells with an EC50 value of 99 nM[2].
|
| ln Vivo |
Fluticasone (1 mg/kg; intranasal instillation; 7 days) decreases rhinovirus-induced airway inflammation in vivo but also inhibits antiviral immune responses and increases viral titers, leading to mucus hypersecretion [4].
|
| Animal Protocol |
Animal/Disease Models: C57BL/6 mice [4]
Doses: 1 mg/kg Route of Administration: intranasal instillation; 1 hour before infection with rhinovirus 1B; 7 days Experimental Results: Inhibition of BAL neutrophil numbers and inhibition of rhinovirus-induced airway inflammation. |
| References |
[1]. Seidel P, et al. Thiazolidinediones inhibit airway smooth muscle release of the chemokine CXCL10: in vitro comparison with current asthma therapies. Respir Res. 2012 Oct 4. 13(1):90.
[2]. Wang J, et al. Identification of select glucocorticoids as Smoothened agonists: potential utility for regenerative medicine. Proc Natl Acad Sci U S A. 2010 May 18. 107(20):9323-8. [3]. Ying Wang, et al. Tiotropium and Fluticasone Inhibit Rhinovirus-Induced Mucin Production via Multiple Mechanisms in Differentiated Airway Epithelial Cells. Front. Cell. Infect. Microbiol., 2020 Jun. [4]. Singanayagam A, et al. Effect of fluticasone propionate on virus-induced airways inflammation and anti-viral immune responses in mice. Lancet. 2015 Feb 26. 385(Suppl 1):S88. |
| Additional Infomation |
Fluticasone is a trifluorinated corticosteroid used in the form of its propionate ester for treatment of allergic rhinitis. It has a role as an anti-allergic agent and an anti-asthmatic drug. It is an 11beta-hydroxy steroid, a 3-oxo-Delta(4) steroid, a corticosteroid, a fluorinated steroid, a 17alpha-hydroxy steroid and a thioester. It derives from a hydride of an androstane.
Fluticasone is a synthetic glucocorticoid available as 2 esters, [DB08906] and [DB00588]. These drugs are available as inhalers, nasal, sprays, and topical treatments for various inflammatory indications. [DB00588] was first approved in 1990 and [DB08906] was approved in 2007. Fluticasone is a Corticosteroid. The mechanism of action of fluticasone is as a Corticosteroid Hormone Receptor Agonist. Fluticasone is a synthetic trifluorinated glucocorticoid receptor agonist with antiallergic, antiinflammatory and antipruritic effects. Fluticasone binds and activates glucocorticoid receptor, resulting in the activation of lipocortin. Lipocortin, in turn, inhibits cytosolic phospholipase A2, which triggers a cascade of reactions involved in the synthesis of inflammatory mediators, such as prostaglandins and leukotrienes. Secondly, mitogen-activated protein kinase (MAPK) phosphatase 1 is induced, thereby leads to dephosphorylation and inactivation of Jun N-terminal kinase directly inhibiting c-Jun mediated transcription. Finally, transcriptional activity of nuclear factor (NF)-kappa-B is blocked, thereby inhibits the transcription of cyclooxygenase 2, which is essential for prostaglandin production. Fluticasone's 2 esters are indicated as inhalers for the treatment and management of asthma by prophylaxisas well as inflammatory and pruritic dermatoses. A [DB00588] nasal spray is indicated for managing nonallergic rhinitis while the [DB08906] nasal spray is indicated for treating season and perennial allergic rhinitis. |
| Molecular Formula |
C22H27F3O4S
|
|---|---|
| Molecular Weight |
444.51
|
| Exact Mass |
500.18441
|
| Elemental Analysis |
C, 59.45; H, 6.12; F, 12.82; O, 14.40; S, 7.21
|
| CAS # |
90566-53-3
|
| Related CAS # |
Fluticasone (propionate);80474-14-2
|
| PubChem CID |
5311101
|
| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
| Density |
1.3±0.1 g/cm3
|
| Boiling Point |
568.3±50.0 °C at 760 mmHg
|
| Melting Point |
-18.1ºC
|
| Flash Point |
297.5±30.1 °C
|
| Vapour Pressure |
0.0±3.5 mmHg at 25°C
|
| Index of Refraction |
1.556
|
| LogP |
3.73
|
| tPSA |
105.97
|
| SMILES |
FCSC([C@]1([C@H](C)C[C@H]2[C@@H]3C[C@H](F)C4=CC(C=C[C@]4(C)[C@@]3(F)[C@H](C[C@]12C)O)=O)O)=O
|
| InChi Key |
MGNNYOODZCAHBA-GQKYHHCASA-N
|
| InChi Code |
InChI=1S/C22H27F3O4S/c1-11-6-13-14-8-16(24)15-7-12(26)4-5-19(15,2)21(14,25)17(27)9-20(13,3)22(11,29)18(28)30-10-23/h4-5,7,11,13-14,16-17,27,29H,6,8-10H2,1-3H3/t11-,13+,14+,16+,17+,19+,20+,21+,22+/m1/s1
|
| Chemical Name |
S-(fluoromethyl) (6S,8S,9R,10S,11S,13S,14S,16R,17R)-6,9-difluoro-11,17-dihydroxy-10,13,16-trimethyl-3-oxo-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthrene-17-carbothioate
|
| Synonyms |
fluticasone; 90566-53-3; Fluticasona; Fluticasonum; Fluticaps; Fluticaps (TN); Fluticasone (INN); Fluticasone, Inhaled;
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2497 mL | 11.2483 mL | 22.4967 mL | |
| 5 mM | 0.4499 mL | 2.2497 mL | 4.4993 mL | |
| 10 mM | 0.2250 mL | 1.1248 mL | 2.2497 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.
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