DUN41875

硬脂酰辅酶A去饱和酶1抑制剂（对大鼠酶的IC50=11.8nM）；在0.01、0.1和1µM浓度下，可增加可溶性α-突触核蛋白的四聚化，并减少突变型α-突触核蛋白在表达3K突变型α-突触核蛋白的BE(2)-M17细胞中掺入四聚体；降低以10或30mg/kg剂量喂食低必需脂肪酸饮食的大鼠的血浆油酸与硬脂酸的比率；在以1.9%（v/v）浓度添加到饮用水中时，可减少帕金森氏病3K-3798转基因小鼠在撑杆测试中的转身时间和跌倒次数，增加从转棒上跌落的时间，并提高其在悬线测试中的耐力；降低同一只小鼠大脑皮质体细胞磷酸化α-突触核蛋白聚集体和皮质LAMP-1水平。A stearoyl-CoA desaturase 1 inhibitor (IC50 = 11.8 nM for the rat enzyme); increases tetramerization of soluble α-synuclein and reduces mutant α-synuclein incorporation into tetramers in BE(2)-M17 cells expressing the 3K mutant α-synuclein at 0.01, 0.1, and 1 µM; reduces the plasma ratio of oleic acid to stearic acid in rats fed a low essential fatty acid diet at 10 or 30 mg/kg; reduces the time to turn and the number of falls in the pole test, increases time to fall from the rotarod, and improves endurance in the hanging wire test in the 3K-3798 transgenic mouse model of Parkinson's disease when administered in the drinking water at 1.9% (v/v); reduces cortex somatic aggregates of phosphorylated α-synuclein and cortex levels of LAMP-1 in the brains from the same mice.分子式C17H16F3N5O分子量363.3CC1=C(C(NC2=NN(C)C=C2)=O)N=CN1CC3=CC(C(F)(F)F)=CC=C3