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Platelet-activating factor (PAF) is a pro-inflammatory phospholipid mediator that is rapidly synthesized by lyso-PAF acetyltransferase (lyso-PAFAT) in response to extracellular stimuli. Two types of lyso-PAFAT have been identified: lysophosphatidylcholine acyltransferase (LPCAT)1, which is mostly expressed in the lungs, and LPCAT2, which is expressed in inflammatory cells. TSI-01 is a selective inhibitor of LPCAT2 (IC₅₀s = 0.47 versus 3.02 μM for human LPCAT2 and LPCAT1, respectively). At 60 μM it was shown to suppress PAF biosynthesis in mouse peritoneal macrophages stimulated with a calcium ionophore.

TSI-01 is a selectve inhibitor of LPCAT2, a platelet-activiating factor acetyltransferase (PAFAT) which acts as a pro-inflammatory phospholipid mediator. Inhibition leads to suppression of PAF biosynthesis.

[1] MEGUMI TARUI. Selective inhibitors of a PAF biosynthetic enzyme lysophosphatidylcholine acyltransferase 2.[J]. Journal of Lipid Research, 2014, 55 7: 1386-1396. DOI: 10.1194/jlr.m049205