Difluprednate

Catalog No.S4095 Batch:S409503

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Technical Data

Formula

C27H34F2O7

Molecular Weight 508.55 CAS No. 23674-86-4
Solubility (25°C)* In vitro DMSO 100 mg/mL (196.63 mM)
Ethanol 100 mg/mL (196.63 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Difluprednate (difluoroprednisolone butyrate acetate, DFBA, CM 9155) 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 (from reference)

Selleck's Difluprednate has been cited by 1 publication

Development and validation of a high-performance liquid chromatography method for the quantification of talazoparib in rat plasma: Application to plasma protein binding studies [ Biomed Chromatogr, 2018, 32(2)] PubMed: 28677821

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.