| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Glucocorticoid receptor (NR3C1).
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|---|---|
| ln Vitro |
Isoflupredone is a potent glucocorticoid receptor agonist. It binds to the glucocorticoid receptor with high affinity, leading to the activation of glucocorticoid response elements (GREs) and the regulation of gene expression. This results in the inhibition of pro-inflammatory mediators (cytokines, chemokines, prostaglandins, leukotrienes) and the suppression of immune cell function. The compound exhibits potent anti-inflammatory, immunosuppressive, and vasoconstrictive activities.
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| ln Vivo |
In horses, isoflupredone significantly lowers the serum potassium level. A powerful medication for treating horses with recurrent airway blockage is isoflupredone[1].
In vivo, isoflupredone exhibits potent anti-inflammatory and immunosuppressive effects. It is used in veterinary medicine for the treatment of various inflammatory conditions, including arthritis, bursitis, tenosynovitis, dermatitis, and allergic reactions. It reduces inflammation, pain, and swelling. The compound is administered by injection or topical application. Its effects are dose-dependent and duration of action is related to its pharmacokinetic properties. |
| Enzyme Assay |
Glucocorticoid receptor binding affinity is measured using radioligand binding assays. The glucocorticoid receptor is incubated with a radiolabeled ligand (e.g., ³H-dexamethasone) and varying concentrations of isoflupredone. Competitive binding is measured and the IC₅₀ or Ki value is calculated. Transactivation activity is assessed using reporter gene assays in cells transfected with a GRE-luciferase construct. Cells are treated with isoflupredone and luciferase activity is measured.
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| Cell Assay |
Cell-based assays for glucocorticoid activity use cell lines expressing the glucocorticoid receptor (e.g., A549, HeLa). Cells are treated with isoflupredone at various concentrations. Glucocorticoid receptor activation is assessed by measuring the expression of glucocorticoid-responsive genes (e.g., GILZ, MKP-1) by qPCR or Western blot. Anti-inflammatory activity is assessed by measuring the inhibition of LPS-induced cytokine production (TNF-α, IL-6, IL-1β) in macrophage cell lines.
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| Animal Protocol |
In vivo studies are typically conducted in animal models of inflammation. In veterinary applications, isoflupredone is used in dogs, cats, and horses for the treatment of inflammatory conditions. Efficacy is assessed by clinical signs (reduction in swelling, pain, lameness). Pharmacokinetic studies are conducted in target animal species following administration by various routes. Tissue distribution and elimination are assessed.
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| ADME/Pharmacokinetics |
Isoflupredone is a glucocorticoid with typical pharmacokinetic properties of this class. It is rapidly absorbed after injection, has moderate protein binding, and is metabolized in the liver. It is eliminated in urine and feces. The duration of action is related to the dose and route of administration. Specific pharmacokinetic data for isoflupredone are available from veterinary pharmacology studies. It is intended for veterinary and research use.
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| Toxicity/Toxicokinetics |
Isoflupredone is a synthetic glucocorticoid with potent anti-inflammatory properties. As with other glucocorticoids, prolonged use or high doses can lead to adverse effects, including immunosuppression, adrenal suppression, osteoporosis, and metabolic disturbances. It should be used with caution in animals with infections, diabetes, or other systemic diseases. The compound is intended for veterinary use and research applications only.
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| References |
[1]. Picandet V, et al. Comparison of efficacy and tolerability of isoflupredone and dexamethasone in the treatment of horses affected with recurrent airway obstruction ('heaves'). Equine Vet J. 2003;35(4):419-424.
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| Additional Infomation |
9-Fluoroprednisolone is a 21-hydroxysteroid.
See also: Isoflurane acetate (active ingredient). Isoflupredone is a fluorinated synthetic glucocorticoid used primarily in veterinary medicine for its potent anti-inflammatory and immunosuppressive properties. It is a derivative of prednisolone with enhanced potency due to the 9α-fluorine substitution. The compound is used for the treatment of inflammatory conditions such as arthritis, dermatitis, and allergic reactions in animals. It is also used as a reference standard for pharmaceutical analysis and quality control of glucocorticoid-containing products. It is for veterinary and research use only. |
| Molecular Formula |
C21H27FO5
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|---|---|
| Molecular Weight |
378.43
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| Exact Mass |
378.184
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| CAS # |
338-95-4
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| PubChem CID |
127516
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
566.7±50.0 °C at 760 mmHg
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| Melting Point |
274 - 275ºC
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| Flash Point |
296.5±30.1 °C
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| Vapour Pressure |
0.0±3.5 mmHg at 25°C
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| Index of Refraction |
1.600
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| LogP |
1.38
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
27
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| Complexity |
775
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| Defined Atom Stereocenter Count |
7
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| SMILES |
OCC(C1(CCC2C3CCC4=CC(C=CC4(C)C3(F)C(CC12C)O)=O)O)=O
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| InChi Key |
WAIJIHDWAKJCBX-BULBTXNYSA-N
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| InChi Code |
InChI=1S/C21H27FO5/c1-18-7-5-13(24)9-12(18)3-4-15-14-6-8-20(27,17(26)11-23)19(14,2)10-16(25)21(15,18)22/h5,7,9,14-16,23,25,27H,3-4,6,8,10-11H2,1-2H3/t14-,15-,16-,18-,19-,20-,21-/m0/s1
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| Chemical Name |
(8S,9R,10S,11S,13S,14S,17R)-9-fluoro-11,17-dihydroxy-17-(2-hydroxyacetyl)-10,13-dimethyl-6,7,8,11,12,14,15,16-octahydrocyclopenta[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) |
DMSO: 25 mg/mL (66.06 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.50 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. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.50 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.50 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 | 2.6425 mL | 13.2125 mL | 26.4250 mL | |
| 5 mM | 0.5285 mL | 2.6425 mL | 5.2850 mL | |
| 10 mM | 0.2642 mL | 1.3212 mL | 2.6425 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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