Potent and selective cytosolic phospholipase A2 alpha (cPLA2α) inhibitor (IC50 = 20 nM). Selective for cPLA2α over secreted PLA2α (sPLA2α; exhibits no inhibition at 10 μM). Inhibits cPLA2α-dependent inflammatory responses in vitro in guinea pig and human whole-blood assays. Improves diet-induced liver injury and CCl4-induced hepatic fibrosis in vivo. Orally bioavailable.
XT2 is a highly potent, orally active, and selective inhibitor of NF-κB-inducing kinase (NIK), exhibiting an IC50 of 9.1 nM. It effectively suppresses the upregulation of ALT, a vital biomarker for acute liver injury, induced by CCl4. Additionally, XT2 significantly decreases immune cell infiltration into the damaged liver tissue. As a result, XT2 holds immense potential in liver inflammatory disease research [1].
8,12-iso-iPF2α-VI, an isoprostane, arises from non-enzymatic, free radical-induced peroxidation of membrane lipids. It is the predominant isoprostane formed during lipid peroxidation and serves as a biomarker for oxidative stress. Detectable in hepatic tissue post CCl4-induced oxidative damage, 8,12-iso-iPF2α-VI levels are also elevated in the urine, blood, and cerebrospinal fluid of Alzheimer’s disease patients.