GKT136901

NOX1和NOX4的双重抑制剂（Kis分别为160和165nM）；对NOX1和NOX4具有选择性，优于NOX2和黄嘌呤氧化酶（Kis分别为1,530和>30,000nM），以及10µM的18种酶和离子通道；在0.1、1和10µM的无细胞测定中，清除过氧亚硝酸盐自由基，并防止α-突触核蛋白的硝化和二聚体的形成；在10µM时，防止过氧亚硝酸盐诱导的分化LUHMES细胞死亡。A dual inhibitor of NOX1 and NOX4 (Kis = 160 and 165 nM, respectively); selective for NOX1 and NOX4 over NOX2 and xanthine oxidase (Kis = 1,530 and >30,000 nM, respectively), as well as a panel of 18 enzymes and ion channels at 10 µM; scavenges peroxynitrite radicals, as well as prevents the nitration and dimer formation of α-synuclein, in cell-free assays at 0.1, 1, and 10 µM; prevents peroxynitrite-induced cell death of differentiated LUHMES cells at 10 µM.分子式C19H15ClN4O2分子量366.8O=C1C=C2NN(C3=C(Cl)C=CC=C3)C(C2=C(C)N1CC4=CC=CC=N4)=O