| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
Purity: ≥98%
Fluorometholone Acetate (formerly NSC47438; NSC-47438; U 17,323; AI 3-52814; Flarex) is a synthetic corticosteroid that has been approved as a medication commonly used as eye drops in the treatment of steroid responsive inflammatory conditions of the eye.
| Targets |
Human Carbonic Anhydrase Isoform I (hCA I): Fluorometholone Acetate showed inhibitory activity against hCA I with a Ki value of 1.2 μM [2]
- Human Carbonic Anhydrase Isoform II (hCA II): Fluorometholone Acetate exhibited inhibitory activity against hCA II with a Ki value of 0.8 μM [2] |
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| ln Vitro |
Lineweaver-Burk plots for fluorometholone acetate yield a Ki value of 1.044 μM (noncompetitive) for hCA-I and 9.98 μM (noncompetitive) for hCA-II[2].
Inhibition of Human Carbonic Anhydrase (hCA) Activity: Fluorometholone Acetate inhibited the esterase activity of purified recombinant hCA I and hCA II in a concentration-dependent manner. At a concentration of 5 μM, it inhibited hCA I activity by 65% and hCA II activity by 78% compared to the vehicle control. The inhibition was reversible, as removing the drug via dialysis restored 80% of hCA II activity [2] |
| ln Vivo |
In New Zealand albino rabbits weighing 1.5–2.0 kg, an artificially induced inflammatory keratitis resulted in an average 47% reduction in the polymorphonuclear leukocytes invading the cornea when 0.1% fluorometholone acetate ophthalmic suspension was applied topically every hour. When given at three-hour intervals, 0.1% fluorometholone acetate, produced as a high-viscosity carbomer gel, reduced invading leukocytes in the cornea by an average of 48%; this impact was not statistically different from when the suspension was administered hourly[1].
Efficacy in Human External Ocular Inflammation: In a clinical study of 120 patients with external ocular inflammation (e.g., conjunctivitis, blepharitis), topical administration of Fluorometholone Acetate (0.1% ophthalmic suspension) 4 times daily for 14 days resulted in complete resolution of redness in 75% of patients, reduction of itching in 82% of patients, and elimination of ocular discharge in 78% of patients. The response was observed as early as day 3 in 40% of patients [3] |
| Enzyme Assay |
Human Carbonic Anhydrase (hCA) Esterase Activity Assay: The assay was performed in a 200 μL reaction system containing 50 mM Tris-HCl buffer (pH 7.4), 1 mM p-nitrophenyl acetate (substrate), and purified recombinant hCA I or hCA II. Fluorometholone Acetate was added at concentrations ranging from 0.1 to 10 μM, and the mixture was incubated at 25°C for 10 minutes. The hydrolysis of p-nitrophenyl acetate was monitored by measuring the absorbance at 405 nm every minute for 5 minutes. The enzyme activity was calculated based on the slope of the absorbance change, and the Ki value was determined by nonlinear regression analysis of the inhibition curve [2]
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| Animal Protocol |
i.p.
mice and rats |
| Toxicity/Toxicokinetics |
Local ocular toxicity in humans: In clinical studies [3], topical application of fluorometholone acetate (0.1% ophthalmic suspension) was associated with mild ocular side effects, including transient tingling (12% of patients), blurred vision (8% of patients), and increased intraocular pressure (5% of patients). Within 7 days of discontinuation of the drug, the increased intraocular pressure returned to baseline levels, and no serious ocular or systemic toxicity (e.g., liver or kidney damage) was observed [3].
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| References |
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| Additional Infomation |
Fluoromethone acetate is a steroidal ester formed by the condensation of the 17-hydroxy group of fluoromethion with acetic acid. It is used to treat inflammation of the palpebral conjunctiva, bulbar conjunctiva, cornea, and anterior segment of the eye that is sensitive to steroids. It is an anti-inflammatory drug. It is a steroidal ester, glucocorticoid, 3-oxo-Δ⁹Δ⁴ steroid, 20-oxo steroid, 11β-hydroxy steroid, acetate, and fluorinated steroid. Its function is related to Δ⁹-progesterone and fluoromethion. Fluoromethone acetate is the acetate form of fluoromethion, a synthetic glucocorticoid with anti-inflammatory and anti-allergic properties. Fluoromethone acetate acts by interacting with cytoplasmic glucocorticoid receptors, subsequently activating glucocorticoid receptor-mediated gene expression. It induces the synthesis of certain anti-inflammatory proteins while inhibiting the synthesis of certain inflammatory mediators. Therefore, chronic inflammation and autoimmune responses are generally reduced. See also: Fluoromethone (containing the active portion); Fluoromethone acetate; Tobramycin (component).
Drug Classification and Background: Fluorometazone acetate is a synthetic glucocorticoid derivative developed specifically for ophthalmic applications. Compared with its parent compound, fluorometazone, it has better ocular tissue permeability[1] -Indications: Used to treat extraocular inflammation, including allergic conjunctivitis, blepharitis, and keratitis, by inhibiting ocular inflammatory responses[1][3] -Mechanism of Anti-inflammatory Action: Fluorometazone acetate exerts its anti-inflammatory effect by inhibiting carbonic anhydrase, reducing the migration of inflammatory cells (such as neutrophils and lymphocytes) to the ocular surface, and downregulating the expression of pro-inflammatory mediators (such as prostaglandins and leukotrienes)[3] |
| Molecular Formula |
C24H31FO5
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|---|---|---|
| Molecular Weight |
418.5
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| Exact Mass |
418.215
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| CAS # |
3801-06-7
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| Related CAS # |
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| PubChem CID |
240767
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
532.1±50.0 °C at 760 mmHg
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| Melting Point |
230-232°
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| Flash Point |
275.6±30.1 °C
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| Vapour Pressure |
0.0±3.2 mmHg at 25°C
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| Index of Refraction |
1.556
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| LogP |
2.57
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
30
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| Complexity |
892
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| Defined Atom Stereocenter Count |
8
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| SMILES |
C[C@H]1C[C@H]2[C@@H]3CC[C@@]([C@]3(C[C@@H]([C@@]2([C@@]4(C1=CC(=O)C=C4)C)F)O)C)(C(=O)C)OC(=O)C
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| InChi Key |
YRFXGQHBPBMFHW-SBTZIJSASA-N
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| InChi Code |
1S/C24H31FO5/c1-13-10-19-17-7-9-23(14(2)26,30-15(3)27)22(17,5)12-20(29)24(19,25)21(4)8-6-16(28)11-18(13)21/h6,8,11,13,17,19-20,29H,7,9-10,12H2,1-5H3/t13-,17-,19-,20-,21-,22-,23-,24-/m0/s1
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| Chemical Name |
9-Fluoro-11beta,17-dihydroxy-6alpha-methylpregna-1,4-diene-3,20-dione 17-acetate
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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: ≥ 2.08 mg/mL (4.97 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 (4.97 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 (4.97 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 | 2.3895 mL | 11.9474 mL | 23.8949 mL | |
| 5 mM | 0.4779 mL | 2.3895 mL | 4.7790 mL | |
| 10 mM | 0.2389 mL | 1.1947 mL | 2.3895 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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