Difluprednate

SKU: orb1300739

Description

Difluprednate is a potent synthetic corticosteroid used in ophthalmic research. It is primarily applied in studies of post-surgical ocular inflammation and pain, serving as a key pharmacological tool in both in vitro assays and in vivo animal models of inflammatory eye disease.

Research Area

Metabolism Research

Key Properties

• CAS Number: 23674-86-4
• MW: 508.55
• Purity: 99.86% (May vary between batches)
• Formula: C₂₇H₃₄F₂O₇
• SMILES: [H][C@@]12CC[C@](OC(=O)CCC)(C(=O)COC(C)=O)[C@@]1(C)C[C@H](O)[C@@]1(F)[C@@]2([H])C[C@H](F)C2=CC(=O)C=C[C@]12C
• Target: Phospholipase,Others
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.93 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:50 mg/mL (98.32 mM);Ethanol:24 mg/mL (47.19 mM)

Bioactivity

• 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%).
• 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). 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, Epitopic, inhibit, Myser, Difluprednate, CM9155, CM-9155, CM 9155, Phospholipase

Compound Identifiers

PubChem CID

443936