| 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 | |||
| Other Sizes |
| 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. |
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| 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. |
| 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.
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| Molecular Formula |
C27H34F2O7
|
|---|---|
| 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
|
| 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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