Flumethasone
Based on 1 publication(s) in Google Scholar
Flumethasone (Flumetasone) is an orally active, high selective and potent glucocorticoid receptor (GR) agonist. Flumethasone activates GR to inhibit nuclear factor kappa B (NF-κB)-mediated pro-inflammatory cytokine production (TNF-α, IL-1β) and promotes anti-inflammatory gene expression (IL-10), while also regulating metabolic enzyme activity (tyrosine aminotransferase induction). Flumethasone is promising for research of inflammatory diseases, cancer, and endocrine regulation.
For research use only. We do not sell to patients.
- Purity : 99.84%
- CAS No.: 2135-17-3
- Formula: C22H28F2O5
- Molecular Weight:410.45
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) Flumethasone
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Biological Activity
Description
In Vitro
Flumethasone (0-200 nM; 0-24 h) reduces Nrf2 protein levels through glucocorticoid receptor (GCR)-dependent proteasomal degradation in A549 and H460 cells[1].
Flumethasone (100 nM; 4 h) enhances ubiquitination of Nrf2 in A549 and H460 cells, an effect blocked by GCR knockdown[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:A549 and H460 cells
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Concentration:50 nM, 100 nM, 200 nM
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Incubation Time:0-24 h
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Result:Decreased Nrf2 protein levels in a concentration-dependent manner, with significant reduction observed at 100 nM and 200 nM.
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Cell Line:A549 and H460 cells
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Concentration:100 nM
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Incubation Time:4 h
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Result:Promoted Nrf2 ubiquitination, and this effect was abrogated in GCR-knockdown cells.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult male C57BL/6J mice and C57BL/6J-ob obese mutant mice[2]
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Dosage:10-8 to 10-6 moles/kg
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Administration:i.p., a single dose
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Result:Induced a 10-fold increase in liver TA activity at 4 hr, significantly higher than hydrocortisone derivatives in adrenalectomized C57BL/6J mice.
Chemical Information
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CAS No. 2135-17-3
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Appearance Solid
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Molecular Weight 410.45
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Formula C22H28F2O5
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Color White to off-white
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SMILES
C[C@@]12[C@](C(CO)=O)(O)[C@H](C)C[C@@]1([H])[C@]3([H])C[C@H](F)C4=CC(C=C[C@]4(C)[C@@]3(F)[C@@H](O)C2)=O
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Synonyms
Flumetasone
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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 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Drug Test Anal
High-throughput liquid chromatography tandem mass spectrometry assay as initial testing procedure for analysis of total urinary fraction. [Abstract]2021 Feb;13(2):283-298. PMID: 32852861
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (243.64 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.09 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.09 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
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.
Protocols
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RT-PCR
Reverse transcription technology uses RNA as a template to synthesize DNA. RT-PCR is simple, specific and sensitive, and can be used to detect gene expression levels and expression differences in cells; detect RNA virus content; clone cDNA sequences of specific genes.
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
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Real Time qPCR (Q-PCR)
Real-time quantitative PCR (qPCR) quantifies an amplifiable nucleic-acid target by monitoring fluorescence during PCR cycling rather than measuring product only after amplification. The increase in fluorescence tracks accumulation of PCR product, and the quantification cycle (Cq; historically also Ct/CP) is related to the initial amount of target: samples containing more starting target generally reach the defined fluorescence threshold in fewer cycles.
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Pyroptosis Solutions
Pyroptosis is a lytic inflammatory cell-death pathway executed by gasdermin pores, most classically through inflammasome-mediated activation of caspase-1, cleavage of gasdermin D, membrane pore formation, LDH release, and secretion of IL-1β and IL-18. The canonical pathway is commonly modeled by priming cells with an inflammatory signal such as LPS to induce pro-IL-1β and inflammasome components, followed by an activation signal such as ATP or nigericin to activate NLRP3, ASC speck formation, caspase-1 cleavage, GSDMD cleavage, cytokine release, and pyroptotic membrane rupture. The non-canonical pathway is triggered when cytosolic LPS activates mouse caspase-11 or human caspase-4/5, leading to GSDMD cleavage and pyroptosis, and this can secondarily activate NLRP3-dependent IL-1β release. Pyroptosis is linked to inflammatory injury, infection, cancer, liver disease, ocular disease, placental inflammation, and other disease phenotypes, but unresolved questions include which gasdermin fam
Purity & Documentation
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Data Sheet (282 KB)
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SDS (418 KB)
- English - EN (418 KB)
- Français - FR (418 KB)
- Deutsch - DE (418 KB)
- Norwegian - NO (418 KB)
- Español - ES (418 KB)
- Swedish - SV (418 KB)
- Italian - IT (418 KB)
- Korean - KR (418 KB)
- Portuguese - PT (418 KB)
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Handling Instructions (2659 KB)
References
[1]. Zhou Y, et al. Flumethasone enhances the efficacy of chemotherapeutic drugs in lung cancer by inhibiting Nrf2 signaling pathway. Cancer Lett. 2020 Apr 1;474:94-105. [Content Brief]
[2]. Blake RL. Flumethasone induction of liver tyrosine aminotransferase activity in inbred strains and obese mutant mice. Biochem Pharmacol. 1970 May;19(5):1803-15. [Content Brief]
[3]. Bednarek D, et al. The effect of steroidal and non-steroidal anti-inflammatory drugs on the cellular immunity of calves with experimentally-induced local lung inflammation. Vet Immunol Immunopathol. 1999 Oct 1;71(1):1-15. [Content Brief]
[4]. Willi RA, et al. Environmental glucocorticoids corticosterone, betamethasone and flumethasone induce more potent physiological than transcriptional effects in zebrafish embryos. Sci Total Environ. 2019 Jul 1;672:183-191. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4364 mL | 12.1818 mL | 24.3635 mL | 60.9088 mL |
| 5 mM | 0.4873 mL | 2.4364 mL | 4.8727 mL | 12.1818 mL | |
| 10 mM | 0.2436 mL | 1.2182 mL | 2.4364 mL | 6.0909 mL | |
| 15 mM | 0.1624 mL | 0.8121 mL | 1.6242 mL | 4.0606 mL | |
| 20 mM | 0.1218 mL | 0.6091 mL | 1.2182 mL | 3.0454 mL | |
| 25 mM | 0.0975 mL | 0.4873 mL | 0.9745 mL | 2.4364 mL | |
| 30 mM | 0.0812 mL | 0.4061 mL | 0.8121 mL | 2.0303 mL | |
| 40 mM | 0.0609 mL | 0.3045 mL | 0.6091 mL | 1.5227 mL | |
| 50 mM | 0.0487 mL | 0.2436 mL | 0.4873 mL | 1.2182 mL | |
| 60 mM | 0.0406 mL | 0.2030 mL | 0.4061 mL | 1.0151 mL | |
| 80 mM | 0.0305 mL | 0.1523 mL | 0.3045 mL | 0.7614 mL | |
| 100 mM | 0.0244 mL | 0.1218 mL | 0.2436 mL | 0.6091 mL |