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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 (PPARgamma) by LPA has also been reported. Tetradecyl phosphonate is a pan-antagonist of lysophosphatidic acid 1 (LPA1), LPA2, and LPA3 receptors with IC50 values for inhibition of LPA-induced calcium mobilization of 10 µM, 5.5 µM, and 3.1 µM, respectively. At a concentration of 10 µM, tetradecyl phosphonate activates a peroxisome proliferator-activated receptor gamma reporter construct 4-fold compared to controls and partially inhibits autotaxin with an IC50 of approximately 3 µM.