A potent LTA4H inhibitor (Kd = 25 nM; IC50 = 47 nM); also inhibits the aminopeptidase activity of LTA4H (IC50s = 72 -150 nM); does not show inhibitory activity against a panel of more than 50 additional aminopeptidases

DG-051 – 5 mg

Brand:
Cayman
CAS:
929915-58-2
Storage:
-20
UN-No:
De Minimis - 1170 / 3

DG-051 is a potent, orally bioavailable leukotriene A4 hydrolase (LTA4H) inhibitor (Kd = 25 nM; IC50 = 47 nM), the enzyme that catalyzes the rate-determining step in the synthesis of LTB4 (Item No. 20110).{34688} 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; Item No. 11188), respectively, potentially leading to PGP accumulation in vivo.{34688,34689} DG-051 does not show any inhibitory activity against a panel of more than 50 additional aminopeptidases, ion channels, or HERG.{34688}  

 

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Description

A potent LTA4H inhibitor (Kd = 25 nM; IC50 = 47 nM); also inhibits the aminopeptidase activity of LTA4H (IC50s = 72 -150 nM); does not show inhibitory activity against a panel of more than 50 additional aminopeptidases, ion channels, or HERG,

Formal name: (2S)-2-[[4-(4-chlorophenoxy)phenoxy]methyl]-1-pyrrolidinebutanoic acid, monohydrochloride

Synonyms: 

Molecular weight: 426.3

CAS: 929915-58-2

Purity: ≥98%

Formulation: A solution in ethanol

Product Type|Biochemicals|Small Molecule Inhibitors|Peptidases & Proteases||Research Area|Lipid Biochemistry|Lipoxygenase Pathways

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