Home Endocrinology & Hormones Glucocorticoid Receptor agonist Fluticasone propionate

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Fluticasone propionate Glucocorticoid Receptor agonist

Cat.No.S1992

Fluticasone Propionate (CCI-187881) is a synthetic glucocorticoid, used to treat non-allergic and allergic rhinitis.
Fluticasone propionate Glucocorticoid Receptor agonist Chemical Structure

Chemical Structure

Molecular Weight: 500.57

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Quality Control

Batch: S199201 DMSO]100 mg/mL]false]Ethanol]5 mg/mL]false]Water]Insoluble]false Purity: 99.97%
99.97

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (199.77 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 500.57 Formula

C25H31F3O5S

 Storage (From the date of receipt)
CAS No. 80474-14-2 Download SDF Storage of Stock Solutions

Synonyms CCI-187881 Smiles CCC(=O)OC1(C(CC2C1(CC(C3(C2CC(C4=CC(=O)C=CC43C)F)F)O)C)C)C(=O)SCF

Mechanism of Action

Targets/IC50/Ki
Glucocorticoid receptor
In vitro
Fluticasone propionate (1 pM) inhibits the constitutive and TGF-beta-induced expression of alpha-SMA in human lung myofibroblasts. This compound blocks the TNF-alpha-induced nuclear translocation of the pro-inflammatory transcription factor NF-kappaB in human lung myofibroblasts. It inhibits in lung myofibroblasts, at a very early stage of differentiation, the activation of Janus kinase/STAT pathways induced by IL-13 (tyrosine kinase 2, STAT1, STAT3, STAT6, mitogen-activated protein kinase). This chemical still displays a potential anti-inflammatory activity even if it only inhibits tyrosine kinase 2 phosphorylation in mildly or fully differentiated myofibroblastic cultures. It inhibits constitutive and TGF-beta-induced expression of alpha-smooth muscle actin, the main marker of myofibroblastic differentiation, both in very early and in mild differentiated myofibroblasts. This compound displays an additional powerful anti-inflammatory effect, decreasing nuclear translocation of NF-kappaB independent of the degree of myofibroblastic differentiation. It inhibits allergen-induced T-cell proliferation, expression of IL-3, IL-5 and GM-CSF mRNA, and secretion of the corresponding proteins in a concentration-dependent fashion. This chemical has the potential markedly to inhibit allergen-induced T-cell production of asthma-relevant cytokines.
In vivo
Fluticasone propionate administrated after induction of a severe heaves exacerbation results in complete resolution of clinical signs, normalization of pulmonary function tests, and significant decrease in bronchoalveolar lavage (BAL) neutrophilia in horse.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/11943316/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06290102 Recruiting
Asthma
Teva Branded Pharmaceutical Products R&D Inc.
 May 2 2024 Phase 1
NCT02630121 Recruiting
Sleep Apnea|Chronic Nasal Congestion
University of South Florida
 April 2023 Phase 4
NCT05608681 Recruiting
Eosinophilic Esophagitis
Eupraxia Pharmaceuticals Inc.
 March 31 2023 Phase 1|Phase 2

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