Description
DG-051 is a potent, orally bioavailable leukotriene A
4 hydrolase (LTA
4H) inhibitor (K
d = 25 nM; IC
50 = 47 nM), the enzyme that catalyzes the rate-determining step in the synthesis of LTB
4 . However, it also inhibits the aminopeptidase activity of LTA
4H with IC
50 values of 72 and 150 nM when tested using the substrates L-alanine
p-nitroanaline and prolyl-glycyl-proline peptide (PGP; ), respectively, potentially leading to PGP accumulation
in vivo. DG-051 does not show any inhibitory activity against a panel of more than 50 additional aminopeptidases, ion channels, or HERG.
Uses
(2S)?-2-?[[4-?(4-Chlorophenoxy)?phenoxy]?methyl]?-1-?pyrrolidinebutanoic Acid Hydrochloride is a potent inhibitor leukotriene A4 hydrolase (LTA4H), which is a therapeutic target for developing treatments for cardiovascular diseases and cancers.
