Oxylone acetate

Names

[ Name ]:
Oxylone acetate

[Synonym ]:
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

Biological Activity

[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].

[Related Catalog]:

Research Areas >> Inflammation/Immunology

Signaling Pathways >> Metabolic Enzyme/Protease >> Carbonic Anhydrase

[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]

[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].

[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].

[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.

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
532.1±50.0 °C at 760 mmHg

[ Melting Point ]:
230-232°

[ Molecular Formula ]:
C₂₄H₃₁FO₅

[ Molecular Weight ]:
418.498

[ Flash Point ]:
275.6±30.1 °C

[ Exact Mass ]:
418.215546

[ PSA ]:
80.67000

[ LogP ]:
2.57

[ Vapour Pressure ]:
0.0±3.2 mmHg at 25°C

[ Index of Refraction ]:
1.556

Safety Information

[ RIDADR ]:
NONH for all modes of transport

[ HS Code ]:
2942000000

Customs

[ HS Code ]: 2942000000

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.