929915-58-2

DG-051 is a potent, orally bioavailable leukotriene A₄ hydrolase (LTA₄H) inhibitor (K_d = 25 nM; IC₅₀ = 47 nM), the enzyme that catalyzes the rate-determining step in the synthesis of LTB₄ . However, it also inhibits the aminopeptidase activity of LTA₄H with IC₅₀ 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.

(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.

[1] VINCENT SANDANAYAKA. Discovery of 4-[(2S)-2-{[4-(4-Chlorophenoxy)phenoxy]methyl}-1-pyrrolidinyl]butanoic Acid (DG-051) as a Novel Leukotriene A4 Hydrolase Inhibitor of Leukotriene B4 Biosynthesis[J]. Journal of Medicinal Chemistry, 2009, 53 2: 573-585. DOI: 10.1021/jm900838g
[2] CAROLINE M LOW. The development of novel LTA4H modulators to selectively target LTB4 generation.[J]. Scientific Reports, 2017: 44449. DOI: 10.1038/srep44449