compound introduction
TFAP是一种细胞可渗透的吡啶基-苯甲酰胺化合物，通过靶向酶的活性位点，相对于Cox-2（IC | 50 |为210μM），可作为Cox-1（IC0于0.80μM）的选择性抑制剂。 （30 mg / kg，口服）对小鼠和大鼠的体内特性无长期细胞毒性作用（小鼠每天300 mg / kg，口服持续14天）。与抑制Cox-2的止痛药（如阿司匹林）不同，TFAP在体内不会对大鼠造成胃损伤（300 mg / kg，口服）。 TFAP is a cell-permeable pyridinyl-benzamide compound that acts as a Cox-1 (IC|50|of 0.80 μM) selective inhibitor versus Cox-2 (IC|50|of 210 μM) by targeting the enzyme's active site and displays analgesic properties in mice and rats in vivo (30 mg/kg, p.o.) without long-term cytotoxic effects (300 mg/kg in mice, daily, p.o. for 14 days). Unlike Cox-2-inhibiting analgesics such as aspirin, TFAP is shown not to cause gastric damage in rats in vivo (300 mg/kg, p.o.).
