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Fluorometholone acetate

CAS: 3801-06-7 F: C24H31FO5 W: 418.50

Fluorometholone acetate is a synthetic glucocorticoid corticosteroid and a corticosteroid ester. Fluorometholone acetate
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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
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
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.