1345808-25-4

Arginase inhibitor 1 is an inhibitor of arginase I and II (IC₅₀s = 223 and 509 nM, respectively, for the recombinant human enzymes). It decreases arginase I activity in CHOK cells expressing human arginase I (IC₅₀ = 8 μM). Arginase inhibitor 1 (100 mg/kg, i.v.) reduces infarct size in a rat model of myocardial ischemia and reperfusion injury induced by left-main coronary artery occlusion.

Arginase inhibitor 1 is a potent inhibitor of human arginases I and II with IC50s of 223 and 509 nM, respectively.

[1] Van Zandt MC, et al. Discovery of (R)-2-amino-6-borono-2-(2-(piperidin-1-yl)ethyl)hexanoic acid and congeners as highly potentinhibitors of human arginases I and II for treatment of myocardial reperfusion injury. J Med Chem. 2013 Mar 28;56(6):2568-80. DOI:10.1021/jm400014c