Biological Activity
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 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].
References
[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.
