BI-2545 is a potent autotaxin (ATX) inhibitor that significantly reduces LPA, with IC50s of 2.2 nM and 3.4 nM for human ATX and rat ATX, respectively[1].
BI-2545 displays good potency in the LPA and rat whole blood assay with IC50s of 29 nM and 96 nM, respectively[1].
BI-2545 (10 mg/kg; p.o.) has high and sustained in vivo efficacy in reducing LPAs[1].BI-2545 (10 mg/kg; p.o.) has a half-life of t1/2=3.4 hours[1]. Animal Model: Rat[1]
[1]. Kuttruff, C. A., et al. Discovery of BI-2545: A Novel Autotaxin Inhibitor That Significantly Reduces LPA Levels in Vivo. ACS Medicinal Chemistry Letters, 8(12), 1252-1257.