| Name | Difluprednate |
| Description | Difluprednate (Myser)(Durezol) is a corticosteroid, approved for the treatment of post-operative ocular inflammation and pain. |
| 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] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | Ethanol : 24 mg/mL (47.19 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 50 mg/mL (98.32 mM), Sonication is recommended.
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| Keywords | Phospholipase | Inhibitor | inhibit | Difluprednate | CM-9155 | CM9155 |
| Inhibitors Related | Neomycin sulfate | 1-Naphthaleneacetic acid potassium salt | trans-Benzylideneacetone | Benzylideneacetone | Omeprazole | Tris(2,4-di-tert-butylphenyl)phosphate | (E/Z)-Polydatin | Indomethacin | Fluticasone (propionate) | 1-Naphthaleneacetic acid | Darapladib | Lansoprazole |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Bioactive Compound Library | Pain-Related Compound Library | ReFRAME Related Library | Drug Repurposing Compound Library | CNS-Penetrant Compound Library | NO PAINS Compound Library | FDA-Approved Drug Library | Immunology/Inflammation Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Human Metabolite Library |
United States
