| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| 2g | |||
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| Targets |
Glucocorticoid receptor (GR). Difluprednate is a potent glucocorticoid receptor agonist. Upon binding to the glucocorticoid receptor, the compound modulates gene expression through transactivation and transrepression mechanisms, leading to the inhibition of pro-inflammatory cytokines and mediators. The difluorination enhances its potency and receptor binding affinity compared to prednisolone.
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| ln Vitro |
Difluprednate has potent anti-inflammatory activity in vitro. It inhibits the production of pro-inflammatory cytokines such as IL-1, IL-6, and TNF-α in various cell types. The compound shows enhanced potency compared to prednisolone due to its difluorinated structure. In vitro studies demonstrate its ability to suppress inflammatory responses in ocular and other cell types.
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| ln Vivo |
Difluprednate is effective in vivo for the treatment of ocular inflammation and pain following ophthalmic surgery. Clinical studies have demonstrated its efficacy in reducing inflammation and pain in patients undergoing cataract surgery and other ocular procedures. The compound is administered as an ophthalmic emulsion and has shown favorable efficacy and safety profiles in clinical trials.
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| Enzyme Assay |
In vitro glucocorticoid receptor binding assays for Difluprednate are performed using recombinant GR or cytosolic preparations from cells expressing GR. Competitive binding assays using [3H]dexamethasone are used to assess affinity. Transactivation assays using reporter genes (e.g., GRE-luciferase) in GR-expressing cells are used to measure agonist activity. Anti-inflammatory activity is assessed by measuring cytokine production in stimulated cells.
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| Cell Assay |
Cellular assays for Difluprednate are performed using various cell types including ocular cells (e.g., corneal epithelial cells, conjunctival cells) and immune cells. Cells are stimulated with inflammatory stimuli (e.g., LPS, TNF-α) and treated with Difluprednate at varying concentrations. Pro-inflammatory cytokine production is measured by ELISA or qPCR. NF-κB activation is assessed by Western blot or immunofluorescence. Cell viability is monitored to assess cytotoxicity.
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| Animal Protocol |
In vivo animal studies for Difluprednate are performed in models of ocular inflammation, such as laser-induced or surgical models in rabbits or rats. The compound is administered as an ophthalmic emulsion, and clinical signs of inflammation (redness, swelling, discharge) are scored. Inflammatory cell infiltration is assessed by histology. Intraocular pressure is monitored as a safety parameter. Pharmacokinetic studies measure drug levels in ocular tissues.
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Difluprednate penetrates the corneal epithelium rapidly and effectively. Systemic absorption is low. Following a single instillation of labeled Difluprednate into the right eye of a colored rabbit, 78.5% of the radioactive material was excreted within 24 hours and 99.5% within 7 days. Metabolism/Metabolites Difluprednate is rapidly deacetylated in the aqueous humor to difluoroprednisolone butyrate (DFB), the active metabolite of the drug. Endogenous tissue esterases subsequently metabolize DFB to the inert metabolite hydroxyfluoroprednisolone butyrate (HFB), thus limiting systemic exposure to the active compound. Difluprednate has a molecular weight of 508.55 g/mol and molecular formula C27H34F2O7. It is a corticosteroid with low aqueous solubility and is formulated as an ophthalmic emulsion for ocular administration. The compound should be stored at room temperature, protected from light, and should not be frozen. The ophthalmic emulsion is typically supplied in sterile single-use or multi-dose containers. |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation There is currently no information regarding the use of desflurane eye drops during lactation. Due to limited ocular absorption, desflurane eye drops are not expected to have any adverse effects on breastfed infants. To significantly reduce the amount of medication that enters breast milk after instillation, press your finger against the tear duct near the corner of your eye for at least 1 minute, then blot away any excess medication with absorbent paper. ◉ Effects on Breastfed Infants No published information found as of the revision date. ◉ Effects on Breastfeeding and Breast Milk No published information found as of the revision date. Difluprednate has an acceptable safety profile when used as an ophthalmic emulsion. Common adverse effects include increased intraocular pressure, ocular discomfort, and cataract formation with prolonged use. As a corticosteroid, it carries the risk of delayed wound healing and increased susceptibility to infections. Systemic absorption is minimal with ophthalmic administration but should be monitored in patients at risk. |
| References | |
| Additional Infomation |
Difluprednate is a corticosteroid and a butyrate ester. Difluprednate is a topical corticosteroid used to treat inflammation and pain associated with ophthalmic surgery. It is the butyrate ester of 6(α),9(α)-difluoroprednisolone acetate. The abbreviation for Difluprednate is DFBA, which stands for difluoroprednisolone butyrate acetate. It is used to treat endogenous anterior uveitis. Difluprednate is a topical corticosteroid and a derivative of prednisolone acetate with anti-inflammatory activity. After instillation into the eye, Difluprednate binds to and activates the glucocorticoid receptor (GR). The receptor-ligand complex binds to the promoter region of certain genes, initiating RNA transcription. This leads to the induction of the synthesis of phospholipase A2 repressor protein, thereby inhibiting the synthesis of arachidonic acid and blocking the synthesis of certain inflammatory mediators such as prostaglandins and leukotrienes. This can reduce ocular inflammation and pain. Drug Indications For the treatment of inflammation and pain associated with ophthalmic surgery. FDA Label Mechanism of Action Corticosteroids are thought to act by inducing phospholipase A2 to inhibit proteins (lipocortin). These proteins are presumed to control the biosynthesis of potent inflammatory mediators such as prostaglandins and leukotrienes by inhibiting the release of their common precursor, arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A2.
Difluprednate is a potent difluorinated corticosteroid used for the treatment of ocular inflammation and pain following ophthalmic surgery. It is a glucocorticoid receptor agonist with enhanced anti-inflammatory activity compared to prednisolone. Difluprednate is marketed as an ophthalmic emulsion and has been shown to be effective in reducing postoperative inflammation and pain in patients undergoing cataract surgery and other ocular procedures. The compound is for clinical use and is available by prescription. |
| Molecular Formula |
C27H34F2O7
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|---|---|
| Molecular Weight |
508.5515
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| Exact Mass |
508.227
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| CAS # |
23674-86-4
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| PubChem CID |
443936
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
600.3±55.0 °C at 760 mmHg
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| Melting Point |
192 - 194ºC
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| Flash Point |
316.9±31.5 °C
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| Vapour Pressure |
0.0±3.9 mmHg at 25°C
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| Index of Refraction |
1.545
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| LogP |
3.67
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
36
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| Complexity |
1050
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| Defined Atom Stereocenter Count |
8
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| SMILES |
CCCC(=O)O[C@@]1(CC[C@@H]2[C@@]1(C[C@@H]([C@]3([C@H]2C[C@@H](C4=CC(=O)C=C[C@@]43C)F)F)O)C)C(=O)COC(=O)C
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| InChi Key |
WYQPLTPSGFELIB-JTQPXKBDSA-N
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| InChi Code |
InChI=1S/C27H34F2O7/c1-5-6-23(34)36-26(22(33)14-35-15(2)30)10-8-17-18-12-20(28)19-11-16(31)7-9-24(19,3)27(18,29)21(32)13-25(17,26)4/h7,9,11,17-18,20-21,32H,5-6,8,10,12-14H2,1-4H3/t17-,18-,20-,21-,24-,25-,26-,27-/m0/s1
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| Chemical Name |
[(6S,8S,9R,10S,11S,13S,14S,17R)-17-(2-acetyloxyacetyl)-6,9-difluoro-11-hydroxy-10,13-dimethyl-3-oxo-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-17-yl] butanoate
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| Synonyms |
W6309 W-6309 W 6309
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~491.59 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (4.92 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.09 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.09 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9664 mL | 9.8319 mL | 19.6637 mL | |
| 5 mM | 0.3933 mL | 1.9664 mL | 3.9327 mL | |
| 10 mM | 0.1966 mL | 0.9832 mL | 1.9664 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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