tcsc6085 DG051

DG051 is a potent leukotriene A4 hydrolase inhibitor of leukotriene B4 biosynthesis in the enzyme assay with an IC₅₀=47 nM.

IC50 & Target: IC50: 47 nM (LTA4H)^[1]

In Vitro: DG051 is a potent inhibitor of LTA4H aminopeptidase activity against L-alanine p-nitroanilide (IC₅₀=72 nM). DG051 inhibits human whole blood (HWB) with IC₅₀ of 37 nM. As applied within the context of LTA4H inhibitor design, the chemistry team is able to design a potent DG051(K_d=26 nM) with high aqueous solubility (>30 mg/mL) and high oral bioavailability (>80% across species) that is currently undergoing clinical evaluation for the treatment of myocardial infarction and stroke^[1] DG-051 is a first-in-class small molecule inhibitor of leukotriene A4 hydrolase (LTA4H), currently in Phase II clinical development for the prevention of heart attack^[2].