CAY10594 是磷脂酶 D2 抑制剂 (体外IC50=140 nM,细胞IC50=110 nM)。它在体外显著阻碍乳腺癌细胞的侵袭性迁移,并调节磷酸化 GSK-3β/JNK 轴改善扑热息痛诱导的急性肝损伤。
产品描述
CAY10594 is a potent phospholipase D2(PLD2) inhibitor. CAY10594 ameliorates acetaminophen-induced acute liver injury by regulating the phosphorylated-GSK-3β/JNK axis.
体内活性
CAY10594 administration markedly blocked the acute liver injury in a dose-dependent manner, showing almost complete inhibition with 8?mg/kg of CAY10594. During the pathological progress of acute liver injury, GSH levels are decreased, and this is significantly recovered upon the administration of CAY10594 at 6?hours post APAP challenge. GSK-3β (Serine 9)/JNK phosphorylation is mainly involved in APAP-induced liver injury. CAY10594 administration strongly blocked GSK-3β (Serine 9)/JNK phosphorylation in the APAP-induced acute liver injury model. Consistently, sustained JNK activation in the cytosol and mitochondria from hepatocytes were also decreased in CAY10594-treated mice. Many types of immune cells are also implicated in APAP-induced liver injury. However, neutrophil and monocyte populations were not different between vehicle- and CAY10594-administered mice which are challenged with APAP. Therapeutic administration of CAY10594 also significantly attenuated liver damage caused by the APAP challenge, eliciting an enhanced survival rate[1].
动物实验
Mice were fasted for 16?hours before APAP injection. APAP (500?mg/kg) was administered with oral gavage in mice. CAY10594 (N-[2-(4-oxo-1-phenyl-1,3,8-triazaspiro[4,5]dec-8-yl)ethyl]-2-naphthalene carboxamide)23 was dissolved in 1% DMSO and intraperitoneally administered to mice 30?minutes prior to APAP injection for examining protective effects or after 3?hours from APAP challenge for investigating therapeutic effects of CAY10594[1].
Cas No.
1130067-34-3
分子式
C26H28N4O2
分子量
428.5
储存和溶解度
DMSO:20mg/ml(46.7mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years