| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| Other Sizes |
| Targets |
Diflorasone diacetate targets the intracellular glucocorticoid receptor (GR). Following diffusion across the cell membrane, it binds to the cytoplasmic GR, and the receptor complex translocates to the nucleus, where it interacts with glucocorticoid response elements (GREs) in DNA. This results in the upregulation of anti-inflammatory proteins such as lipocortins and IkappaB and the repression of pro-inflammatory cytokines, including IL-1, IL-2, IL-4, IL-6, and macrophage inflammatory protein-2 (MIP-2).
|
|---|---|
| ln Vitro |
In vitro, diflorasone reduces the production of the inflammatory cytokines IL-6, IL-4, and macrophage inflammatory protein-2 (Mip-2). It also acts as an inhibitor of TARC (thymus and activation-regulated chemokine, CCL17) in the dinitrochlorobenzene (DNCB) model. The anti-inflammatory activity is thought to occur through the induction of phospholipase A2 inhibitory proteins collectively called lipocortins, which control the biosynthesis of prostaglandins and leukotrienes.
|
| ln Vivo |
In vivo, topical administration of 20 uL of a 0.05% diflorasone diacetate solution completely inhibits swelling in the ears of toluene-2,4-diisocyanate-sensitized mice. It also alleviates swelling in the ears of sensitized animals and has been shown to be effective in animal models of dermatitis, including the DNCB model. The compound is formulated as a 0.05% cream or ointment for once- or twice-daily application.
|
| Enzyme Assay |
This is not a cell-free biochemical enzyme inhibition assay; rather, diflorasone is a glucocorticoid receptor agonist. Activity is assessed using GR binding assays where the compound is incubated with recombinant GR protein or cytosolic extracts in buffer, followed by the addition of a radiolabeled tracer such as 3H-dexamethasone, to determine binding affinity and displacement.
|
| Cell Assay |
Cellular activity is assessed using primary human keratinocytes or immune cells. Cells are treated with diflorasone diacetate (0.01-10 uM) for 4-24 hours, followed by stimulation with pro-inflammatory stimuli (e.g., LPS or TNF-alpha). Culture supernatants are collected for IL-6, IL-4, TNF-alpha, and MIP-2 measurement by ELISA, while cell lysates are analyzed for NF-kappaB activation and IkappaB levels by Western blot.
|
| Animal Protocol |
Topical corticosteroid efficacy is evaluated in murine models of contact hypersensitivity or acute inflammation such as the DNCB or TDI model. Mice receive topical application of diflorasone diacetate (e.g., 20 uL of 0.05% solution) to the ear or skin. Disease severity is assessed by measuring ear thickness, histological analysis (H&E staining, inflammatory cell infiltration), and tissue cytokine levels (ELISA, qPCR).
|
| ADME/Pharmacokinetics |
Following dermal application, diflorasone diacetate is absorbed through intact skin, with penetration enhanced by inflammation or occlusion. Once absorbed, it follows pharmacokinetic pathways similar to systemically administered corticosteroids, undergoing hepatic metabolism. The 0.05% cream formulation achieves local therapeutic concentrations in the skin with limited systemic exposure, although absorption can be sufficient to produce systemic effects with large-area application or occlusive dressings.
|
| Toxicity/Toxicokinetics |
Diffusely absorbed topical corticosteroids, including diflorasone diacetate, can produce reversible hypothalamic-pituitary-adrenal (HPA) axis suppression, Cushing‘s syndrome, hyperglycemia, and glucosuria in some patients. Pediatric patients may absorb proportionally larger amounts and be more susceptible to systemic toxicity. Application to large surface areas, prolonged use, or occlusive dressings increases risk. Diflorasone has been shown to be teratogenic (cleft palate) in rats at topical doses of approximately 0.001 mg/kg/day.
|
| Additional Infomation |
Diflurasone diacetate is a 17,21-diacetate derivative of diflurasone. It is used topically to treat various skin diseases due to its anti-inflammatory and antipruritic properties. It has anti-inflammatory and antipruritic effects. It is an 11β-hydroxysteroid, glucocorticoid, 20-oxosteroid, fluorosteroid, acetate, and 3-oxo-Δ(1),Δ(4)-steroid. It is functionally related to diflurasone and acetate. It is derived from the hydride of pregnane. Diflurasone diacetate is the acetate form of diflurasone, a synthetic glucocorticoid with anti-inflammatory and immunosuppressive properties. Like other glucocorticoids, diflurasone enters the cell by diffusion across the cell membrane and binds to the glucocorticoid receptor (GR) in the cytoplasm. Subsequently, the receptor complex translocates to the nucleus and activates or inhibits genes by interacting with short palindromic DNA sequences called glucocorticoid response elements (GREs). Gene activation can produce anti-inflammatory effects, such as upregulating IκB; while gene repression inhibits the production of pro-inflammatory cytokines (such as interleukin-1 (IL-1), IL-2, and IL-6), thereby preventing the activation of cytotoxic T lymphocytes.
See also: diflubenzuron (with active fraction). Diflorasone diacetate (brand names include Florone, Maxiflor, Psorcon) is a prescription medication approved for the topical treatment of corticosteroid-responsive dermatoses. It is classified as a high-potency topical corticosteroid with enhanced efficacy due to fluorination at the 6alpha and 9alpha positions and diacetate esterification at the 17 and 21 positions. As an FDA-approved drug, it is commercially available for clinical use but should only be used under medical supervision due to its potency and potential for adrenal suppression. |
| Molecular Formula |
C26H32F2O7
|
|---|---|
| Molecular Weight |
494.53
|
| Exact Mass |
494.211
|
| CAS # |
33564-31-7
|
| PubChem CID |
71414
|
| Appearance |
White to off-white solid powder
|
| Density |
1.3±0.1 g/cm3
|
| Boiling Point |
585.1±50.0 °C at 760 mmHg
|
| Melting Point |
47-49 °C(lit.)
|
| Flash Point |
307.6±30.1 °C
|
| Vapour Pressure |
0.0±3.7 mmHg at 25°C
|
| Index of Refraction |
1.546
|
| LogP |
3.1
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
9
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
35
|
| Complexity |
1050
|
| Defined Atom Stereocenter Count |
9
|
| SMILES |
C[C@H]1C[C@H]2[C@@H]3C[C@@H](C4=CC(=O)C=C[C@]4(C)[C@]3([C@H](C[C@]2(C)[C@]1(C(=O)COC(=O)C)OC(=O)C)O)F)F
|
| InChi Key |
BOBLHFUVNSFZPJ-JOYXJVLSSA-N
|
| InChi Code |
InChI=1S/C26H32F2O7/c1-13-8-17-18-10-20(27)19-9-16(31)6-7-23(19,4)25(18,28)21(32)11-24(17,5)26(13,35-15(3)30)22(33)12-34-14(2)29/h6-7,9,13,17-18,20-21,32H,8,10-12H2,1-5H3/t13-,17-,18-,20-,21-,23-,24-,25-,26-/m0/s1
|
| Chemical Name |
[2-[(6S,8S,9R,10S,11S,13S,14S,16S,17R)-17-acetyloxy-6,9-difluoro-11-hydroxy-10,13,16-trimethyl-3-oxo-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-17-yl]-2-oxoethyl] acetate
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~202.22 mM)
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0221 mL | 10.1106 mL | 20.2212 mL | |
| 5 mM | 0.4044 mL | 2.0221 mL | 4.0442 mL | |
| 10 mM | 0.2022 mL | 1.0111 mL | 2.0221 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
