Fluticasone furoate

Name: Fluticasone furoate
Brand: MedChemExpress
SKU: HY-15234
Rating: 4.5 (0 reviews)

Cat. No.: HY-15234 Purity: 98.90%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

Fluticasone furoate is a topical, intranasal, enhanced-affinity synthetic trifluorinated corticosteroid with a K_d 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.

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Fluticasone furoate 화학구조

CAS No. : 397864-44-7

사이즈	재고	수량

무료 샘플 (0.1 - 0.2 mg)	지금 신청하기
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	해외재고보유	Estimated Time of Arrival: December 31
Solid
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
200 mg	해외재고보유	Estimated Time of Arrival: December 31
500 mg	해외재고보유	Estimated Time of Arrival: December 31
1 g	견적 받기
5 g	견적 받기

or 대량구매 문의

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This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 1 Customer Validation

Other Forms of Fluticasone furoate:

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity
순도&문서
References
고객리뷰

제품 설명

IC₅₀ & Target

Kd: 0.3 nM (Corticosteroid)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
PBMC	IC₅₀	0.05 1 Compound: 3	Inhibition of TNFalpha release in human PBMC by ELISA assay Inhibition of TNFalpha release in human PBMC by ELISA assay	[PMID: 21880489]
PBMC	IC₅₀	0.05 1 Compound: 3	Inhibition of TNFalpha release in human PBMC by ELISA assay Inhibition of TNFalpha release in human PBMC by ELISA assay	[PMID: 21880489]
RAW264.7	IC₅₀	0.1 1 Compound: 1	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	[PMID: 29741897]
RAW264.7	IC₅₀	0.1 1 Compound: 1	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	[PMID: 29741897]
PBMC	IC₅₀	0.05 1 Compound: 3	Inhibition of TNFalpha release in human PBMC by ELISA assay Inhibition of TNFalpha release in human PBMC by ELISA assay	[PMID: 21880489]
RAW264.7	IC₅₀	0.1 1 Compound: 1	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	[PMID: 29741897]
SW1353	EC₅₀	0.49 1 Compound: 3	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	[PMID: 21880489]

In Vitro

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.

In Vivo

Fluticasone furonate is 99.4% bound to plasma protein in vitro and other research indicated extensive first-pass metabolism of the absorbed drug. Protein binding is highly relevant because only the unbound free drug can exert an effect at the receptor site. Clearance of Fluticasone furonate is primarily by hydrolysis in the liver by the cytochrome P450 isozyme (CYP) 3A4 that converts the drug to the 17β-carboxylic acid metabolite (M10), which displays low glucocorticoid receptor agonist potency. Fluticasone furonate is excreted mainly in the feces, with only minor amounts in the urine^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

분자량

538.58

화학식

C₂₇H₂₉F₃O₆S

CAS No.

397864-44-7

Appearance

Solid

Color

White to off-white

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

선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

용액&용해도

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.8567 mL	9.2837 mL	18.5673 mL
5 mM	0.3713 mL	1.8567 mL	3.7135 mL
10 mM	0.1857 mL	0.9284 mL	1.8567 mL

View the 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.

몰농도 계산기
농도 희석 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.64 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

순도&문서

Purity: 98.90%

Select Batch:

Data Sheet (280 KB) SDS (419 KB)

COA (258 KB) HNMR (310 KB) LCMS (96 KB)

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

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