Fluticasone furoate
Based on 1 Customer Validation
Fluticasone furoate is a topical, intranasal, enhanced-affinity synthetic trifluorinated corticosteroid with a Kd of 0.3 nM. Fluticasone furoate has potent anti-inflamatory and anti-asthmatic activity, and low systemic exposure. Fluticasone furoate has the potential for allergic rhinitis treatment.
For research use only. We do not sell to patients.
- Purity: 98.90%
- CAS No.: 397864-44-7
- Formula: C27H29F3O6S
- Molecular Weight:538.58
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Kd: 0.3 nM (Corticosteroid)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| PBMC | IC50 |
0.05 nM
Compound: 3
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Inhibition of TNFalpha release in human PBMC by ELISA assay
Inhibition of TNFalpha release in human PBMC by ELISA assay
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[PMID: 21880489] |
| RAW264.7 | IC50 |
0.1 nM
Compound: 1
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Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide release preincubated for 15 mins followed by LPS challenge measured after 18 hrs by Griess assay
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide release preincubated for 15 mins followed by LPS challenge measured after 18 hrs by Griess assay
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[PMID: 29741897] |
| SW1353 | EC50 |
0.49 nM
Compound: 3
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Agonist activity at GR in human SW1353 cells transfected with luciferase gene linked to MMTV promoter assessed as luciferase transactivation activity
Agonist activity at GR in human SW1353 cells transfected with luciferase gene linked to MMTV promoter assessed as luciferase transactivation activity
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[PMID: 21880489] |
Fluticasone furoate comes in a nasal spray, as an aqueous suspension of micronized fluticasone furoate for topical administration to the nasal mucosa by means of a metering, atomizing spray pump[1].
Fluticasone furonate displays great potency in inhibiting tumor necrosis factor synthesis and action. Fluticasone furonate is also potent in preventing damage to cultured human lung epithelial cells by different stimulus[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 397864-44-7
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Appearance Solid
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Molecular Weight 538.58
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Formula C27H29F3O6S
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Color White to off-white
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SMILES
C[C@@]12[C@](C(SCF)=O)(OC(C3=CC=CO3)=O)[C@H](C)C[C@@]1([H])[C@]4([H])C[C@H](F)C5=CC(C=C[C@]5(C)[C@@]4(F)[C@@H](O)C2)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (185.67 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.64 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
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Handling Instructions (2659 KB)
References
[1]. Giavina-Bianchi P, et al. Fluticasone furoate nasal spray in the treatment of allergic rhinitis. Ther Clin Risk Manag. 2008 Apr;4(2):465-72. [Content Brief]
[2]. Alizadeh Z, et al. Asthma phenotypes and T-bet protein expression in cells treated with Fluticasone Furoate/Vilanterol. Pulm Pharmacol Ther. 2020 Feb;60:101886. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8567 mL | 9.2837 mL | 18.5673 mL | 46.4184 mL |
| 5 mM | 0.3713 mL | 1.8567 mL | 3.7135 mL | 9.2837 mL | |
| 10 mM | 0.1857 mL | 0.9284 mL | 1.8567 mL | 4.6418 mL | |
| 15 mM | 0.1238 mL | 0.6189 mL | 1.2378 mL | 3.0946 mL | |
| 20 mM | 0.0928 mL | 0.4642 mL | 0.9284 mL | 2.3209 mL | |
| 25 mM | 0.0743 mL | 0.3713 mL | 0.7427 mL | 1.8567 mL | |
| 30 mM | 0.0619 mL | 0.3095 mL | 0.6189 mL | 1.5473 mL | |
| 40 mM | 0.0464 mL | 0.2321 mL | 0.4642 mL | 1.1605 mL | |
| 50 mM | 0.0371 mL | 0.1857 mL | 0.3713 mL | 0.9284 mL | |
| 60 mM | 0.0309 mL | 0.1547 mL | 0.3095 mL | 0.7736 mL | |
| 80 mM | 0.0232 mL | 0.1160 mL | 0.2321 mL | 0.5802 mL | |
| 100 mM | 0.0186 mL | 0.0928 mL | 0.1857 mL | 0.4642 mL |
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