| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
Purity: ≥98%
Flumethasone (NSC-54702; RS-2177; U-10974; RS2177; BRN-5645455; NSC54702; Anaprime; Aniprime; Fluvet; Methagon; Cortexilar; Flucort; Flucorticin;Locacorten), a topically used corticosteroid, is a potent glucocorticoid receptor agonist with potential anti-inflammatory activity.
| ln Vitro |
The impact of one single therapeutic dose of flumethasone (0.5 mg/100 kg b.w.) on insulin sensitivity was studied in calves. Hyperinsulinemic, euglycemic clamp tests were performed before and after flumethasone treatment. At 24 h after treatment, insulin-dependent glucose utilization was reduced by 74% (P < 0.005). No significant changes occurred 72 h post-treatment.[1]
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| ln Vivo |
Cows were treated with 500 ml of 50% glucose solution. IV, and 40 mg of dexamethasone, IM (group 1), 40 mg of dexamethasone, IM (group 2), 5 mg of flumethasone (group 3), or 500 ml of 50% glucose solution, IV, and 5 mg of flumethasone (group 4). Treatment success was defined as recovery after a single treatment without relapse during the same lactation. Uterine disease (retained placenta or metritis), parity, and pretreatment plasma glucose, serum beta-hydroxybutyric acid, and urine acetoacetate concentrations were evaluated as possible confounding factors affecting recovery.[2]
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
When applied topically, absorption, distribution, and excretion are minimal. Metabolism/Metabolites Primarily metabolized in the liver. |
| References |
Zentralbl Veterinarmed A.1998 Sep;45(6-7):441-3;J Am Vet Med Assoc.1996 May 15;208(10):1702-4.
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| Additional Infomation |
Flumethasone is a fluorinated corticosteroid belonging to the class of glucocorticoids, 11β-hydroxysteroids, 17α-hydroxysteroids, 21-hydroxysteroids, 20-oxosteroids, 3-oxo-Δ⁹Δ⁴-steroids, primary α-hydroxy ketones, and tertiary α-hydroxy ketones. It is an anti-inflammatory drug derived from the hydrogenation of pregnane. Flumethasone is a moderately potent difluorinated corticosteroid ester with anti-inflammatory, antipruritic, and vasoconstrictive effects. Because it is a salt compound, its anti-inflammatory effect is concentrated at the site of administration. This local application to the lesion site rapidly reduces inflammation, exudation, and itching. It is an anti-inflammatory glucocorticoid used in veterinary clinical practice. See also: Flumethasone pitavaate (its active ingredient)...see more...
Drug Indications For the treatment of contact dermatitis, atopic dermatitis, eczema, psoriasis, diaper rash, and other skin conditions. Mechanism of Action Flumethasone is a glucocorticoid receptor agonist. This complex binds to the cell nucleus, causing activation and inhibition of various genes. The anti-inflammatory effects of corticosteroids are thought to be related to lipocortin, a phospholipase A2 inhibitor that controls the biosynthesis of prostaglandins and leukotrienes by inhibiting arachidonic acid. Corticosteroids suppress the immune system by reducing lymphatic function, decreasing immunoglobulin and complement concentrations, inducing lymphopenia, and interfering with antigen-antibody binding. Flumethasone binds to plasma cortisol transporters, and its activity is enhanced when it is no longer bound to these transporters. Pharmacodynamics Flumethasone pitava is a moderately potent difluorinated corticosteroid ester with anti-inflammatory, antipruritic, and vasoconstrictive effects. As it is a private salt, its anti-inflammatory effect is concentrated at the site of application. This local action at the lesion site rapidly reduces inflammation, exudation, and itching. |
| Molecular Formula |
C22H28F2O5
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| Molecular Weight |
410.45
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| Exact Mass |
410.19
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| CAS # |
2135-17-3
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| Related CAS # |
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| PubChem CID |
16490
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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 |
569.8±50.0 °C at 760 mmHg
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| Melting Point |
237-240ºC
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| Flash Point |
298.4±30.1 °C
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| Vapour Pressure |
0.0±3.6 mmHg at 25°C
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| Index of Refraction |
1.579
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| LogP |
1.61
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
29
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| Complexity |
839
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| Defined Atom Stereocenter Count |
9
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| SMILES |
C[C@@H]1C[C@H]2[C@@H]3C[C@@H](C4=CC(=O)C=C[C@@]4([C@]3([C@H](C[C@@]2([C@]1(C(=O)CO)O)C)O)F)C)F
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| InChi Key |
WXURHACBFYSXBI-GQKYHHCASA-N
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| InChi Code |
InChI=1S/C22H28F2O5/c1-11-6-13-14-8-16(23)15-7-12(26)4-5-19(15,2)21(14,24)17(27)9-20(13,3)22(11,29)18(28)10-25/h4-5,7,11,13-14,16-17,25,27,29H,6,8-10H2,1-3H3/t11-,13+,14+,16+,17+,19+,20+,21+,22+/m1/s1
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| Chemical Name |
(6S,8S,9R,10S,11S,13S,14S,16R,17R)-6,9-difluoro-11,17-dihydroxy-17-(2-hydroxyacetyl)-10,13,16-trimethyl-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-3-one
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.09 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 25.0 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: ≥ 2.5 mg/mL (6.09 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 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.09 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 | 2.4364 mL | 12.1818 mL | 24.3635 mL | |
| 5 mM | 0.4873 mL | 2.4364 mL | 4.8727 mL | |
| 10 mM | 0.2436 mL | 1.2182 mL | 2.4364 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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