80937-31-1

Name	Flosulide
CAS	80937-31-1
Molecular Formula	C16H13F2NO4S
MDL Number	MFCD00866141
Molecular Weight	353.34
MOL File	80937-31-1.mol

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]-

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Chemical Properties

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)

Safety Data

Symbol(GHS)	GHS07
Signal word	Warning
Hazard statements	H302-H315-H319-H335
Precautionary statements	P261-P305+P351+P338

Hazard Information

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

Supplier

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