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CAY10594
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CAY10594图片
CAS NO:1130067-34-3
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
1 mL*10 mM(in DMSO)电议

产品介绍
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