| Identification | Back Directory | [Name]
Flosulide | [CAS]
80937-31-1 | [Synonyms]
ZK-38997
CGP-28238
CGP-28328
Flosulide
N-[1-Oxo-6-(2,4-difluorophenoxy)indan-5-yl]methanesulfonamide
N-[[6-(2,4-Difluorophenoxy)-2,3-dihydro-1-oxo-1H-inden]-5-yl]methanesulfonamide
Methanesulfonamide, N-[6-(2,4-difluorophenoxy)-2,3-dihydro-1-oxo-1H-inden-5-yl]- | [Molecular Formula]
C16H13F2NO4S | [MDL Number]
MFCD00866141 | [MOL File]
80937-31-1.mol | [Molecular Weight]
353.34 |
| Chemical Properties | Back Directory | [Melting point ]
156 °C(Solv: ethanol (64-17-5)) | [Boiling point ]
446.9±55.0 °C(Predicted) | [density ]
1.506±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [pka]
6.95±0.20(Predicted) |
| Hazard Information | Back Directory | [Uses]
Flosulide is a potent and selective COX-2 inhibitor, used for the treatment for inflammatory diseases. | [in vivo]
In normovolemic rats, flosulide increases renal plasma flow (RPF) and and glomerular filtration rate (GFR). In hypovolemic rats, flosulide (5-25 mg/kg) reduces RPF and GFR. Flosulide at 5 mg/kg reduces 6-keto-PGF1alpha whereas at 25 mg/kg and after indomethacin at 10 mg/kg a fall in 6-keto-PGF1alpha and TXB2 appeares[1]. Flosulide (0.75 mg/day) significantly reduces proteinuria as compared to aspirin treatment. Plasma protein and albumin levels are significantly lower in the aspirin-treated group than in flosulide-treated rats[3]. | [IC 50]
COX-2 | [References]
[1] Turull A, et al. Acute effects of the anti-inflammatory cyclooxygenase-2 selective inhibitor, flosulide, on renal plasma flow and glomerular filtration rate in rats. Inflammation. 2001 Apr;25(2):119-28. DOI:10.1023/a:1007122706770
[2] Zimmermann KC, et al. Cyclooxygenase-2 expression in human esophageal carcinoma. Cancer Res. 1999 Jan 1;59(1):198-204. PMID:9892207
[3] Heise G, et al. Different actions of the cyclooxygenase 2 selective inhibitor flosulide in rats with passive Heymann nephritis. Nephron. 1998 Oct;80(2):220-6. DOI:10.1159/000045171 |
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