AM095 (free acid) is a potent LPA1 receptor antagonist with IC50 values of 0.98 μM for recombinant human LPA1 and 0.73 μM for recombinant mouse LPA1.

LPA1 (mouse):0.73 μM , LPA1 (human):0.98 μM

In vitro, AM095 was a potent LPA receptor antagonist because it inhibited GTPγS binding to Chinese hamster ovary (CHO) cell membranes overexpressing recombinant human or mouse LPA with IC values of 0.98 and 0.73 μM, respectively, and exhibited no LPA agonism. In functional assays, AM095 inhibited LPA-driven chemotaxis of CHO cells overexpressing mouse LPA (IC = 778 nM) and human A2058 melanoma cells (IC = 233 nM)[3].

In vivo, AM095: 1) had high oral bioavailability and a moderate half-life and was well tolerated at the doses tested in rats and dogs after oral and intravenous dosing, 2) dose-dependently reduced LPA-stimulated histamine release, 3) attenuated bleomycin-induced increases in collagen, protein, and inflammatory cell infiltration in bronchalveolar lavage fluid, and 4) decreased kidney fibrosis in a mouse unilateral ureteral obstruction model[3].