BI-2545 is an inhibitor of autotaxin (IC50s = 2.2 and 3.4 for the human and rat enzyme, respectively).1 It is selective for autotaxin over a panel of 48 enzymes, transporters, ion channels, and receptors at 10 ?M. BI-2545 (10 mg/kg) reduces plasma lysophosphatidic acid (LPA) levels in rats.
1.Kuttruff, C.A., Ferrara, M., Bretschneider, T., et al.Discovery of BI-2545: A novel autotaxin inhibitor that significantly reduces LPA levels in vivoACS Med. Chem. Lett.8(12)1252-1257(2017)
















