Lysophosphatidic acid -LPA) is a lipid signalling molecule formed by the hydrolysis of lysophosphatidyl choline by lysophospholipase D, also known as autotaxin -ATX). LPA signals through four different G protein-coupled receptors, LPA1/EDG-2, LPA2/EDG-4, LPA3/EDG-7, and LPA4/GPR23. Activation of peroxisome proliferator-activated receptor .gamma. -PPAR.gamma.) by LPA has also been reported. Tetradecyl phosphonate is a pan-antagonist of LPA1, LPA2, and LPA3 receptors with IC50 values for inhibition of LPA-induced calcium mobilization of 10 uM, 5.5 uM, and 3.1 uM, respectively. At a concentration of 10 uM, tetradecyl phosphonate activates a PPAR.gamma. reporter construct 4-fold compared to controls and partially inhibits ATX with an IC50 of approximately 3 uM.
產(chǎn)品描述
A pan-antagonist of LPA1-3 receptors -IC50 = 10, 5.5, and 3.1 uM, respectively)