Background:

AM095 is a novel, potent and orally bioavailable antagonist of lysophosphatidic acid type 1 receptor (LPA1) with IC50 values of 0.73 and 0.98 μM for mouse or recombinant human LPA1, respectively [1].

In vitro, AM095 has shown to?inhibit LPA1-induced chemotaxis of both mouse LPA1/CHO cells and human A2058 melanoma cells with IC50 values of 0.78 μM and 0.23μM [1].

In vivo, AM095 could dose-dependently block LPA-induced histamine release with an ED50 value of 8.3 mg/kg in mice. Additionally, AM095 has been revealed to remarkably reduce the BALF collagen and protein with an ED50 value of 10 mg/kg in lungs. AM095 has also shown to decrease both macrophage and lymphocyte infiltration induced by bleomycin in mice [1].

参考文献:
[1] Swaney JS1,?Chapman C,?Correa LD,?Stebbins KJ,?Broadhead AR,?Bain G,?Santini AM,?Darlington J,?King CD,?Baccei CS,?Lee C,?Parr TA,?Roppe JR,?Seiders TJ,?Ziff J,?Prasit P,?Hutchinson JH,?Evans JF,?Lorrain DS. Pharmacokinetic and pharmacodynamic characterization of an oral lysophosphatidic acid type 1 receptor-selective antagonist. J Pharmacol Exp Ther.?2011 Mar;336(3):693-700.