| Description | Fluorometholone acetate is a synthetic glucocorticoid corticosteroid and a corticosteroid ester. Fluorometholone acetate potently inhibits carbonic anhydrase (CA) with IC50s of 2.18 μM and 17.5 μM for hCA-I and hCA-II, respectively. Fluorometholone acetate has anti-inflammatory effect and has the potential for external ocular inflammation research[1][2][3]. |
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| Related Catalog | Research Areas >>Inflammation/ImmunologySignaling Pathways >>Metabolic Enzyme/Protease >>Carbonic Anhydrase |
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| Target | IC50: 2.18 μM (human carbonic anhydrase (hCA)-I) and 17.5 μM (hCA-II)[2] Ki: 1.044 μM (hCA-I) and 9.98 μM (hCA-II)[2] |
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| In Vitro | For Fluorometholone acetate, a Ki value from Lineweaver-Burk plots is obtained as 1.044 μM (noncompetitive) for hCA-I and 9.98 μM (non-competitive) for hCA-II[2]. |
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| In Vivo | Hourly topical administration of 0.1% Fluorometholone acetate ophthalmic suspension produced, on the average, a 47% reduction in the polymorphonuclear leukocytes invading the cornea during an experimentally induced inflammatory keratitis in New Zealand albino rabbits (1.5-2.0 kg). Fluorometholone acetate (0.1%) formulated as a high-viscosity carbomer gel and applied at three-hour intervals reduced invading leukocytes in the cornea an average of 48%, an effect not significantly different from hourly administration of the suspension[1]. |
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| References | [1]. A Kupferman, et al. Fluorometholone acetate. A new ophthalmic derivative of fluorometholone. Arch Ophthalmol. 1982 Apr;100(4):640-1. [2]. Zuhal Alım, et al. Some Anti-Inflammatory Agents Inhibit Esterase Activities of Human Carbonic Anhydrase Isoforms I and II: An In Vitro Study. Chem Biol Drug Des. 2015 Oct;86(4):857-63. [3]. H M Leibowitz, et al. Fluoro metholone acetate: clinical evaluation in the treatment of external ocular inflammation. Ann Ophthalmol. 1984 Dec;16(12):1110-5. |
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| Oxylone acetate |
| (6S,8S,9R,10S,11S,13S,14S,17R)-17-acetyl-9-fluoro-11-hydroxy-6,10,13-trimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-17-yl acetate |
| FLUOROMETHOLONE ACETATE |
| acétate de (6S,8S,9R,10S,11S,13S,14S,17R)-17-acétyl-9-fluoro-11-hydroxy-6,10,13-triméthyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodécahydro-3H-cyclopenta[a]phénanthrén-17-yle |
| [(6S,8S,9R,10S,11S,13S,14S,17R)-17-acetyl-9-fluoro-11-hydroxy-6,10,13-trimethyl-3-oxo-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-17-yl] acetate |
| (6S,8S,9R,10S,11S,13S,14S,17R)-17-Acetyl-9-fluor-11-hydroxy-6,10,13-trimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-17-ylacetat |
| Pregna-1,4-diene-3,20-dione, 17-(acetyloxy)-9-fluoro-11-hydroxy-6-methyl-, (6α,11β)- |
| (6α,11β)-9-Fluoro-11-hydroxy-6-methyl-3,20-dioxopregna-1,4-dien-17-yl acetate |