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

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Quality Control

Batch: Purity: 99.96%

99.96

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Solubility

In vitro
Batch:

DMSO : 100 mg/mL (196.63 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	508.55	Formula	C₂₇H₃₄F₂O₇	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	23674-86-4	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	CM 9155			Smiles	CCCC(=O)OC1(CCC2C1(CC(C3(C2CC(C4=CC(=O)C=CC43C)F)F)O)C)C(=O)COC(=O)C

Mechanism of Action

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). This compound's 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.
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 this compound is instilled in the right eyes of pigmented rabbits in a separate study examining DFBA excretion. This emulsion (0.05%) results in higher aqueous humor concentrations than the suspension form in the eyes of rabbits. Its 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. It suppresses uveitis in all three concentration (0.002%, 0.01%, and 0.05%) in a dose-dependent manner in rats, and this compound 0.05% shows statistically superior anti-inflammatory activity compared to Betamethasone (0.1%).
References	[1] https://pubmed.ncbi.nlm.nih.gov/19668594/ [2] https://pubmed.ncbi.nlm.nih.gov/21750615/

Clinical Trial Information

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

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
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

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Difluprednate

Chemical Structure

Molecular Weight: 508.55