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| Cas No.: | 116686-15-8 |
| Chemical Name: | Methanesulfonamide,N-[4-acetyl-2-(2,4-difluorophenoxy)phenyl]- |
| Synonyms: | Methanesulfonamide,N-[4-acetyl-2-(2,4-difluorophenoxy)phenyl]-;COX-2 Inhibitor V, FK3311;FK 3311;FK-3311;N-[4-acetyl-2-(2,4-difluorophenoxy)phenyl]methanesulfonamide;COX-2 INHIBITOR V;N-[4-Acetyl-2-(2,4-difluorophenoxy)phenyl]-methanesulfonamide FK3311 |
| SMILES: | FC1=CC=C(OC2=C(NS(=O)(C)=O)C=CC(C(C)=O)=C2)C(F)=C1 |
| Formula: | C15H13F2NO4S |
| M.Wt: | 341.33 |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | FK 3311 is a selective inhibitor of COX-2; antiinflammatory agent.IC50 Value: 1.6 uM [1]Target: COX-2Cyclooxygenase (COX) is an intracellular enzyme that converts arachidonic acid into prostaglandin (PG)G2 and PGH2.in vitro: The racemic mixtures and the (R)- and (S)-isomers of the 2 metabolites were inactive in the PGE2 test. IC50 values were more than 100 uM for (2 and 5), compared to 1.6 uM for FK-3311. Antiinflammatory activity was assessed by inhibition of adjuvant-induced arthritis, and analgesic activity was determined in the acetic acid-induced writhing assay. Following p.o. administration of 10 mg/kg, racemic (2) and its optical isomers showed activity comparable to FK-3311 (76% inhibition) in the adjuvant arthritis test, whereas racemic (5) showed very weak activity, and (R)- and (S)-(5) were not tested. With regard to analgesic effects, FK-3311 and racemic (2) showed 81 and 62% inhibitions, respectively, at a dose of 100 mg/kg p.o. The (R)- and (S)-isomers of (2) and racemic (5) all showed 46% inhibition of writhing syndrome. (R)- and (S)-(5) were less active showing 16 and 20% inhibitions, respectively[1].in vivo: L-PVR, CO, PaO(2), and WDR were significantly (P < 0.05) better in the FK group than in the control group. Histological tissue edema was mild, and PMN infiltration was significantly (P < 0.05) reduced in the FK group compared to the control group. The serum TxB(2) levels were significantly (P < 0.05) lower in the FK group than in the control group, while 6-keto-PGF(1alpha) levels were not significantly (P < 0.05) reduced. Two-day survival rate was significantly (P < 0.05) better in the FK group than in the control group [2]. Survival rate was significantly better (p <. 05) and serum GOT levels 30 min after reperfusion were significantly lower (p <. 05) in the FK high-dose group compared to the other two groups. Four hours after reperfusion, GPT levels and liver tissue flow were significantly (p <. 05) better in the FK high-dose group compared to the control. Both 30 min and 4 hr after reperfusion, serum TxB(2) levels were significantly lower in the FK high-dose group compared to the control (p <. 05) [3]. |