| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
Isoflupredone Acetate targets the glucocorticoid receptor. As a corticosteroid with both glucocorticoid and mineralocorticoid activity, it binds to the glucocorticoid receptor and modulates gene expression through transactivation and transrepression mechanisms. This leads to potent anti-inflammatory and gluconeogenic activities. The compound also has mineralocorticoid effects that can affect electrolyte balance.
|
|---|---|
| ln Vitro |
Low concentrations of isofluradone acetate (10-4, 10-7, or 10-10 M; 48 or 96 hours) decrease IL-1β. The effects of 1β (10-7 M and 10-10 M) on inflammation and catabolism are larger than those at high concentrations (10-4 M) [1].
In vitro, Isoflupredone Acetate demonstrates potent topical anti-inflammatory activity. As a glucocorticoid, it inhibits the production of pro-inflammatory cytokines and mediators such as prostaglandins and leukotrienes. The compound's fluorination at the 9-position enhances its potency compared to non-fluorinated corticosteroids. |
| ln Vivo |
Isoflurdone acetate (0.05 mg/kg; IM; days 2 and 4 postchallenge) reduces the reduction in dry matter intake and average daily weight gain and induces hemolytic Mannheimia when paired with oxytetracycline. Clinical improvement in Heimia infection is faster [2].
In vivo, Isoflupredone Acetate is used as a veterinary therapeutic agent with potent anti-inflammatory activity. It is used for the treatment of ketosis, musculoskeletal disorders, hypersensitivity, infections, and inflammatory diseases in cows, horses, pigs, and other large animals. However, it has been shown to increase the frequency of severe hypokalemia in healthy cows. |
| Enzyme Assay |
The in vitro receptor binding assay for Isoflupredone Acetate involves measuring its affinity for the glucocorticoid receptor. Competitive binding assays are performed using radiolabeled dexamethasone or other glucocorticoid ligands. The compound's potency is determined by its ability to displace the labeled ligand from the receptor.
|
| Cell Assay |
Cellular assays for Isoflupredone Acetate are performed using glucocorticoid-responsive cell lines. Cells are treated with the compound at varying concentrations, and glucocorticoid receptor-mediated gene expression is assessed by measuring the expression of target genes such as GILZ or MKP-1. Anti-inflammatory activity is assessed by measuring the inhibition of cytokine production in stimulated cells.
|
| Animal Protocol |
Animal/Disease Models: 96 weaned heifers (bronchopneumonia was induced by intrabronchial infusion of Mannheimia haemolytica) [2]
Doses: 0.05 mg/kg Route of Administration: intramuscularinjection; days 2 and 4 after challenge Experimental Results: Infection resulted in diminished dry matter intake and average daily gain (ADG) in heifers. When combined with oxytetracycline, these reductions are prevented and result in faster clinical improvement. In vivo animal studies for Isoflupredone Acetate are conducted in veterinary species including cows, horses, and pigs. The compound is administered by injection or topically. Efficacy is assessed by measuring clinical signs of inflammation, pain, or disease resolution. Safety studies monitor electrolyte levels, particularly potassium, due to the risk of hypokalemia. |
| ADME/Pharmacokinetics |
Isoflupredone Acetate is administered parenterally or topically in veterinary medicine. As a corticosteroid, it has relatively rapid onset of action. The compound is metabolized in the liver and excreted by the kidneys. Specific PK parameters such as half-life, bioavailability, and clearance are not detailed in the available sources.
|
| Toxicity/Toxicokinetics |
Isoflupredone Acetate has dose-dependent toxicity related to its corticosteroid activity. Adverse effects include hypokalemia (low blood potassium), which can be severe in cows. Other potential side effects include immunosuppression, delayed wound healing, and exacerbation of infections. The compound should be used with caution in animals with diabetes, renal impairment, or infections.
|
| References |
[1]. Trahan RA, et al. In vitro effects of three equimolar concentrations of methylprednisolone acetate, triamcinolone acetonide, and isoflupredone acetate on equine articular tissue cocultures in an inflammatory environment. Am J Vet Res. 2018 Sep;79(9):933-940.
[2]. Hewson J, et al. Impact of isoflupredone acetate treatment on clinical signs and weight gain in weanling heifers with experimentally induced Mannheimia haemolytica bronchopneumonia. Am J Vet Res. 2011 Dec;72(12):1613-21. |
| Additional Infomation |
9α-Fluoro-11β,17α,21-Trihydroxypregn-1,4-diene-3,20-dione 21-acetate is a corticosteroid hormone. See also: Isoflurane (contains the active ingredient); Isoflurane acetate; Neomycin sulfate (one of the components)... See more...
Isoflupredone Acetate is a veterinary corticosteroid used for the treatment of inflammatory conditions in large animals. It is available as a pharmaceutical product for veterinary use and is also available from chemical suppliers for research purposes. The compound is not approved for human use. It serves as a potent anti-inflammatory agent in veterinary medicine. |
| Molecular Formula |
C23H29FO6
|
|---|---|
| Molecular Weight |
420.47
|
| Exact Mass |
420.194
|
| CAS # |
338-98-7
|
| PubChem CID |
224246
|
| Appearance |
White to off-white solid powder
|
| Density |
1.3±0.1 g/cm3
|
| Boiling Point |
576.5±50.0 °C at 760 mmHg
|
| Melting Point |
244-246 °C
|
| Flash Point |
302.5±30.1 °C
|
| Vapour Pressure |
0.0±3.6 mmHg at 25°C
|
| Index of Refraction |
1.577
|
| LogP |
2.46
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
30
|
| Complexity |
879
|
| Defined Atom Stereocenter Count |
7
|
| SMILES |
CC(=O)OCC(=O)[C@]1(CC[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@]3([C@H](C[C@@]21C)O)F)O
|
| InChi Key |
ZOCUOMKMBMEYQV-GSLJADNHSA-N
|
| InChi Code |
InChI=1S/C23H29FO6/c1-13(25)30-12-19(28)22(29)9-7-16-17-5-4-14-10-15(26)6-8-20(14,2)23(17,24)18(27)11-21(16,22)3/h6,8,10,16-18,27,29H,4-5,7,9,11-12H2,1-3H3/t16-,17-,18-,20-,21-,22-,23-/m0/s1
|
| Chemical Name |
[2-[(8S,9R,10S,11S,13S,14S,17R)-9-fluoro-11,17-dihydroxy-10,13-dimethyl-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 |
| 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 : ~125 mg/mL (~297.29 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 | 2.3783 mL | 11.8915 mL | 23.7829 mL | |
| 5 mM | 0.4757 mL | 2.3783 mL | 4.7566 mL | |
| 10 mM | 0.2378 mL | 1.1891 mL | 2.3783 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
