| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 100mg | |||
| Other Sizes |
| Targets |
The primary target of Fluocortolone is the glucocorticoid receptor (GR). It binds to the glucocorticoid receptor, leading to alterations in gene expression that ultimately result in decreased inflammation and immune response. By binding to glucocorticoid receptors, Fluocortolone modulates the transcription of anti-inflammatory genes and represses the expression of pro-inflammatory mediators. It also inhibits progesterone 3α-hydroxysteroid dehydrogenase in rat cortical homogenates with an IC₅₀ of 40 µM. The glucocorticoid receptor is a member of the nuclear receptor superfamily and plays a central role in mediating the effects of corticosteroids.
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| ln Vitro |
In vitro, Fluocortolone inhibits progesterone 3α-hydroxysteroid dehydrogenase activity in rat cortical homogenates with an IC₅₀ value of 40 µM. This enzymatic inhibition demonstrates the compound's ability to interfere with steroid metabolism pathways in neural tissues. Fluocortolone exhibits glucocorticoid receptor binding activity, which can be assessed in receptor binding assays using radiolabeled ligands. The compound's anti-inflammatory activity in vitro can be evaluated by measuring its ability to inhibit the production of pro-inflammatory cytokines such as TNF-α, IL-1β, and IL-6 in activated immune cells.
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| ln Vivo |
In vivo, Fluocortolone demonstrates potent anti-inflammatory activity in animal models. In a rat model of adjuvant-induced joint inflammation, Fluocortolone (3, 6, and 12 mg/kg) significantly inhibits Mycobacterium butyricum-induced foot edema. The compound is orally active and effectively reduces plasma fibrinogen levels. Its anti-inflammatory effects are mediated through glucocorticoid receptor activation, leading to the suppression of pro-inflammatory mediators such as prostaglandins and cytokines. The compound has been investigated for conditions including dermatitis, colitis, and other immune-related disorders.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for Fluocortolone typically involve glucocorticoid receptor binding studies using radioligand competition assays. Receptor binding affinity can be determined by incubating the compound with glucocorticoid receptor preparations and a radiolabeled tracer such as [³H]-dexamethasone, followed by filtration or scintillation counting to measure bound radioactivity. IC₅₀ values are calculated from competition curves. Enzyme inhibition assays for progesterone 3α-hydroxysteroid dehydrogenase can be performed using rat cortical homogenates with appropriate substrates and cofactors, measuring enzymatic activity spectrophotometrically. These protocols are for research purposes only.
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| Cell Assay |
In vitro cell-based assays for Fluocortolone include glucocorticoid receptor-mediated gene expression assays using reporter cell lines transfected with glucocorticoid response element (GRE)-driven luciferase constructs. Cells are treated with Fluocortolone at various concentrations (typically 0.01-100 µM) for 24-48 hours, followed by luciferase activity measurement. Anti-inflammatory activity can be assessed in lipopolysaccharide (LPS)-stimulated macrophages or peripheral blood mononuclear cells by measuring cytokine production (e.g., TNF-α, IL-6) via ELISA. Cell viability assays (MTT or CCK-8) are performed to evaluate cytotoxicity. Standard cell culture conditions (37°C, 5% CO₂) are used with appropriate media and serum supplementation.
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| Animal Protocol |
In vivo animal studies for Fluocortolone utilize the rat adjuvant-induced arthritis model. Male rats are injected with Mycobacterium butyricum in Freund's adjuvant to induce paw edema. Fluocortolone is administered orally at doses of 3, 6, or 12 mg/kg. Paw volume is measured using a plethysmometer at various time points post-treatment. Edema inhibition is calculated as a percentage compared to vehicle-treated controls. Alternative models include carrageenan-induced paw edema and oxazolone-induced dermatitis. Animals are monitored for body weight, clinical signs, and inflammatory parameters. All procedures must comply with institutional animal care guidelines.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Fluocortolone include oral bioavailability and effective plasma fibrinogen reduction. As a glucocorticoid, it is absorbed following oral administration and distributes to target tissues. The compound undergoes hepatic metabolism via cytochrome P450 enzymes, primarily CYP3A4, and is excreted in urine and feces. The half-life in plasma is typically several hours, consistent with other corticosteroids. Fluocortolone binds to plasma proteins, mainly corticosteroid-binding globulin and albumin. Its anti-inflammatory effects are sustained through genomic mechanisms involving transcriptional regulation. Detailed pharmacokinetic parameters may vary depending on the formulation and route of administration.
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| Toxicity/Toxicokinetics |
Toxicological data for Fluocortolone are consistent with those of other glucocorticoids. Chronic use of corticosteroids can lead to adrenal suppression, osteoporosis, hyperglycemia, immunosuppression, and Cushing's syndrome. In animal studies, the compound is well-tolerated at anti-inflammatory doses (3-12 mg/kg). Common adverse effects include fluid retention, weight gain, and increased susceptibility to infections. The compound is for research use only and not for human therapeutic applications. Long-term toxicity studies may be required for clinical development, including assessment of effects on bone density, glucose metabolism, and hypothalamic-pituitary-adrenal axis function.
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| Additional Infomation |
Fluocinolone is a 21-hydroxysteroid. Fluocinolone is a topical corticosteroid with anti-inflammatory activity, used to treat various skin conditions.
Additional information: Fluocortolone is a glucocorticoid that has been investigated for its anti-inflammatory properties. Its mechanism of action involves binding to glucocorticoid receptors, leading to alterations in gene expression that decrease inflammation and immune response. The compound has been studied in the context of various inflammatory conditions including dermatitis and colitis. Fluocortolone is not currently approved for clinical use in major markets and is available only for research purposes. The compound should be stored at -20°C and is soluble in chloroform, methanol, and water. |
| Molecular Formula |
C22H29FO4
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|---|---|
| Molecular Weight |
376.47
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| Exact Mass |
376.204
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| CAS # |
152-97-6
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| PubChem CID |
9053
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
537.4±50.0 °C at 760 mmHg
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| Melting Point |
113-116ºC
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| Flash Point |
278.8±30.1 °C
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| Vapour Pressure |
0.0±3.2 mmHg at 25°C
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| Index of Refraction |
1.572
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| LogP |
1.86
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
27
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| Complexity |
743
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| Defined Atom Stereocenter Count |
9
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| SMILES |
OCC([C@H]1[C@H](C)C[C@H]2[C@@H]3C[C@H](F)C4=CC(C=C[C@]4(C)[C@H]3[C@H](C[C@]12C)O)=O)=O
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| InChi Key |
GAKMQHDJQHZUTJ-ULHLPKEOSA-N
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| InChi Code |
InChI=1S/C22H29FO4/c1-11-6-14-13-8-16(23)15-7-12(25)4-5-21(15,2)20(13)17(26)9-22(14,3)19(11)18(27)10-24/h4-5,7,11,13-14,16-17,19-20,24,26H,6,8-10H2,1-3H3/t11-,13+,14+,16+,17+,19-,20-,21+,22+/m1/s1
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| Chemical Name |
(6S,8S,9S,10R,11S,13S,14S,16R,17S)-6-fluoro-11-hydroxy-17-(2-hydroxyacetyl)-10,13,16-trimethyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthren-3-one
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| 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 | 2.6563 mL | 13.2813 mL | 26.5625 mL | |
| 5 mM | 0.5313 mL | 2.6563 mL | 5.3125 mL | |
| 10 mM | 0.2656 mL | 1.3281 mL | 2.6563 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03757078 | Completed | Drug: Relief Pro cream Drug: Relief Pro rectal suppositories |
Acute Hemorrhoids | Bayer | 2018-11-30 | |
| NCT04358770 | Completed | Drug: Clocortolone Pivalate | Bioequivalence Study | Taro Pharmaceuticals USA | 2018-03-02 | Phase 1 |
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