Difluprednate

Catalog No.S4095 Synonyms: CM 9155

Difluprednate Chemical Structure

Molecular Weight(MW): 508.55

Difluprednate (difluoroprednisolone butyrate acetate, or DFBA) is a synthetic difluorinated prednisolone derivative, it is originally developed for dermatologic applications.

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Biological Activity

Description Difluprednate (difluoroprednisolone butyrate acetate, or DFBA) is a synthetic difluorinated prednisolone derivative, it is originally developed for dermatologic applications.
In vitro

The difluprednate emulsion formulation begin by suspending DFBA in a variety of oils (castor, cottonseed, medium-chain fatty acid triglyceride, oleic, olive, peanut, and soybean). [1] Difluprednate ophthalmic emulsion's active metabolite, 6α,9-difluoroprednisolone 17-butyrate (DFB), has the lowest Ki value (611 nM) for the glucocorticoid receptor and is significantly more active than prednisolone, which has a Ki value of 3.4 nM. [2]

In vivo Difluprednate emulsion is rapidly deacetylated in the aqueous humor to difluoroprednisolone butyrate (DFB) in rats and rabbits, the drug’s active metabolite, which has a similar corticosteroid activity profile. Radio-labeled difluprednate is instilled in the right eyes of pigmented rabbits in a separate study examining DFBA excretion. Difluprednate (0.05% emulsion) results in higher aqueous humor concentrations than the suspension form in the eyes of rabbits. Difluprednate concentrations ≥0.01% shows a statistically significant inhibition of inflammation compared to saline in a rabbit model, with the anti-inflammatory response proceeding in a dose-dependent manner. Difluprednate suppresses uveitis in all three concentration (0.002%, 0.01%, and 0.05%) in a dose-dependent manner in rats, and difluprednate 0.05% shows statistically superior anti-inflammatory activity compared to Betamethasone (0.1%). [1]

Protocol

Solubility (25°C)

In vitro DMSO 100 mg/mL (196.63 mM)
Ethanol 25 mg/mL (49.15 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 508.55
Formula

C27H34F2O7

CAS No. 23674-86-4
Storage powder
in solvent
Synonyms CM 9155

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03693989 Not yet recruiting Cataract Laboratorios Sophia S.A de C.V. October 1 2018 Phase 3
NCT03693989 Not yet recruiting Cataract Laboratorios Sophia S.A de C.V. October 1 2018 Phase 3
NCT01939691 Recruiting Uveitis|Macular Edema University of California San Francisco|Aravind Eye Hospitals India September 12 2018 Phase 4
NCT01939691 Recruiting Uveitis|Macular Edema University of California San Francisco|Aravind Eye Hospitals India September 12 2018 Phase 4
NCT01276223 Completed Dry Eye Disease Alcon Research February 2011 Phase 2
NCT01276223 Completed Dry Eye Disease Alcon Research February 2011 Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID