Difluprednate

Name: Difluprednate
Brand: Selleck Chemicals
SKU: S4095
Rating: 5 (1 reviews)

Synonyms: CM 9155

Catalog No.S4095 Purity:99.96%

Difluprednate (difluoroprednisolone butyrate acetate, DFBA, CM 9155) is a synthetic difluorinated prednisolone derivative, it is originally developed for dermatologic applications.

Difluprednate Chemical Structure

CAS No. 23674-86-4

Purity & Quality Control

Batch: Purity: 99.96%

99.96

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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
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 K_i value of 3.4 nM. ^[2]

In Vivo
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]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT00616993	Completed	Inflammation	Sirion Therapeutics Inc.	January 2008	Phase 3
NCT00616070	Completed	Inflammation	Sirion Therapeutics Inc.	December 2007	Phase 3
NCT00407225	Completed	Inflammation	Sirion Therapeutics Inc.	December 1999	Phase 2
NCT00430092	Completed	Inflammation	Sirion Therapeutics Inc.		Phase 3
NCT00429923	Completed	Inflammation	Sirion Therapeutics Inc.		Phase 3

References

Chemical Information & Solubility

Molecular Weight	508.55	Formula	C₂₇H₃₄F₂O₇
CAS No.	23674-86-4	SDF	Download Difluprednate SDF
Smiles	CCCC(=O)OC1(CCC2C1(CC(C3(C2CC(C4=CC(=O)C=CC43C)F)F)O)C)C(=O)COC(=O)C
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (196.63 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molecular Weight Calculator

In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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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