敏感性 | 易吸湿 |
溶解性 | Soluble in ethanol (78 mg/ml at 25 °C), DMF (40 mg/ml), DMSO (100 mg/ml), PBS (pH 7.2) (~0.5 mg/ml), and water (<1 mg/ml at 25 °C), DMSO 25mg/ml Ethanol dimethyl formamide |
存贮条件 | 储存温度-20°C |
应用 | A highly specific non-competitive inhibitor of NAMPT |
产品介绍 | FK866 (APO866, Daporinad)有效抑制烟酰胺磷酸核糖转移酶(NMPRTase),无细胞试验中IC50为0.09 nM。Phase 1/2。 |
备注 | APO866 effectively inhibits nicotinamide phosphoribosyltransferase (NMPRTase) with IC50 of 0.09 nM. Phase 1/2. |
生化机理 | FK-866 has been shown to induce apoptosis by non-competitive, and specific inhibition of nicotamide phosphoribosyltransferase (NAMPT). NAMPT is a key regulatory enzyme that mediates NAD+ biosynthesis within cells. Mechanistic studies show that this compound contains an enzymatic active site of visfatin which is optimized for nicotinamide binding and inhibition. Visfatin also contains a similar structure to insulin and mimics its actions by binding to the insulin receptors. |
别名 | (2E)-N-[4-(1-苯甲酰基-4-哌啶基)丁基]-3-(3-吡啶基)-2-丙烯酰胺;Daporinad; APO866; FK-866; FK 866; APO 866; APO-866;(E)-N-[4-(1-benzoylpiperidin-4-yl)butyl]-3-(pyridin-3-yl)acrylamide |