N-[4-Acetyl-2-(2,4-difluorophenoxy)phenyl]-methanesulfonamide FK3311
FK 3311
CAS: 116686-15-8
Molecular Formula: C15H13F2NO4S
N-[4-Acetyl-2-(2,4-difluorophenoxy)phenyl]-methanesulfonamide FK3311 - Names and Identifiers
N-[4-Acetyl-2-(2,4-difluorophenoxy)phenyl]-methanesulfonamide FK3311 - Physico-chemical Properties
| Molecular Formula | C15H13F2NO4S |
| Molar Mass | 341.33 |
| Density | 1.419±0.06 g/cm3(Predicted) |
| Boling Point | 431.3±55.0 °C(Predicted) |
| Solubility | 10 mM in DMSO |
| Appearance | White solid |
| pKa | 6.82±0.10(Predicted) |
| Storage Condition | Store at RT |
| In vitro study | Cyclooxygenase (COX) is an intracellular enzyme that converts arachidonic acid into prostaglandin (PG)G2 and PGH2. 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 (COX-2 Inhibitor V). 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. |
| In vivo study | L-PVR, CO, PaO(2), and WDR were significantly better in the FK group than in the control group. Histological tissue edema was mild, and PMN infiltration was significantly reduced in the FK group compared to the control group. The serum TxB(2) levels were significantly lower in the FK group than in the control group, while 6-keto-PGF(1alpha) levels were not significantly reduced. Two-day survival rate was significantly better in the FK group than in the control group. Survival rate was significantly better and serum GOT levels 30 min after reperfusion were significantly lower in the FK high-dose group compared to the other two groups. Four hours after reperfusion, GPT levels and liver tissue flow were significantly 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. |
N-[4-Acetyl-2-(2,4-difluorophenoxy)phenyl]-methanesulfonamide FK3311 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.93 ml | 14.649 ml | 29.297 ml |
| 5 mM | 0.586 ml | 2.93 ml | 5.859 ml |
| 10 mM | 0.293 ml | 1.465 ml | 2.93 ml |
| 5 mM | 0.059 ml | 0.293 ml | 0.586 ml |
Last Update：2024-01-02 23:10:35
N-[4-Acetyl-2-(2,4-difluorophenoxy)phenyl]-methanesulfonamide FK3311 - Reference Information
| biological activity | FK-3311 (COX-2 Inhibitor V) is a selective, cell permeable, oral cyclooxygenase-2 (COX-2) inhibitor with anti-inflammatory effects. FK-3311 can significantly inhibit TxA2 to protect liver febrile ischemia reperfusion injury. |
| target | TargetValue COX-2 () TxA2 () |
| Target | Value |
| in vitro study | Cyclooxygenase (COX) is an intracellular enzyme that converts arachidonic acid into prostaglandin (PG)G2 and PGH2. 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 (COX-COX-2 Inhibitor V). Antiinflammatory activity was assessed by inhibition of adjuvant-induced arthritis, and analgesic activity was determined in the acid-induced writhing say. 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 examined. 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. |
| in vivo studies | L-PVR, CO, PaO(2), and WDR were significantly better in the FK group than in the control group. Histological issue edema was meild, and PMN infiltration was significantly reduced in the FK group compared to the control group. The series TxB(2) levels were significantly lower in the FK group than in the control group, while 6-keto-PGF(1alpha) levels were not significantly reduced. Two-day survival rate was significantly better in the FK group than in the control group. Survival rate was significantly better and serum GOT levels 30 min after reperfusion were significantly lower in the FK high-dose group compared to the other two groups. Four hours after reperfusion, GPT levels and liver tissue flow were significantly 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. |
Last Update：2024-04-09 20:52:54
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CAS: 116686-15-8
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QQ: 3008007409
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CAS: 116686-15-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
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