N-[4-乙酰基-2-(2,4-二氟苯氧基)苯基]-甲烷磺酰胺

生物活性靶点体外研究体内研究 N-[4-乙酰基-2-(2,4-二氟苯氧基)苯基]-甲烷磺酰胺试剂级价格

CAS号:116686-15-8
英文名:FK-3311
中文名:N-[4-乙酰基-2-(2,4-二氟苯氧基)苯基]-甲烷磺酰胺
CBNumber:CB91247805
分子式:C15H13F2NO4S
分子量:341.33
MOL File:116686-15-8.mol

N-[4-乙酰基-2-(2,4-二氟苯氧基)苯基]-甲烷磺酰胺化学性质

沸点 :431.3±55.0 °C(Predicted)
密度 :1.419±0.06 g/cm3(Predicted)
储存条件 :Store at RT
溶解度 :Soluble in DMSO
形态 :White solid
酸度系数(pKa) :6.82±0.10(Predicted)
颜色 :Light yellow to yellow

N-[4-乙酰基-2-(2,4-二氟苯氧基)苯基]-甲烷磺酰胺性质、用途与生产工艺

生物活性 FK-3311 (COX-2 Inhibitor V)是选择性的、细胞可渗透的、口服 cyclooxygenase-2 (COX-2) 抑制剂，具有抗炎作用。FK-3311 可通过显著抑制 TxA2 来对肝热性缺血再灌注损伤起到保护作用。
靶点
Target Value
COX-2
()
TxA2
()
体外研究

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.
体内研究

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.