Bioactivity | 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]. | |||||||||
Target | IC50: 2.18 μM (human carbonic anhydrase (hCA)-I) and 17.5 μM (hCA-II)Ki: 1.044 μM (hCA-I) and 9.98 μM (hCA-II) | |||||||||
Invitro | 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]. | |||||||||
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]. | |||||||||
Name | Fluorometholone acetate | |||||||||
CAS | 3801-06-7 | |||||||||
Formula | C24H31FO5 | |||||||||
Molar Mass | 418.50 | |||||||||
Appearance | Solid | |||||||||
Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
Storage |
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Reference | [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. |