DG051

Names

[ Name ]:
DG051

[Synonym ]:
4-{(S)-2-[4-(4-Chloro-phenoxy)-phenoxymethyl]-pyrrolidin-1-yl}-butyric acid hydrochloride
4-{(2S)-2-[4-(4-chlorophenoxy)phenoxymethyl]pyrrolidin-1-yl}butyric acid hydrochloride
4-{(S)-2-[4-(4-chlorophenoxy)phenoxymethyl]pyrrolidin-1-yl}butyric acid hydrochloride
DG-051 HYDROCHLORIDE
DG051

Biological Activity

[Description]:

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

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Aminopeptidase

Research Areas >> Metabolic Disease

[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(Kd=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].

[References]

[1]. Sandanayaka V, et al. 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 Med Chem. 2010 Jan 28;53(2):573-85.

[2]. Enache LA, et al. Synthesis and structural assignment of two major metabolites of the LTA4H inhibitor DG-051. Bioorg Med Chem Lett. 2009 Nov 15;19(22):6275-9.

[Related Small Molecules]

Ubenimex | Tosedostat

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₁H₂₅Cl₂NO₄

[ Molecular Weight ]:
426.33400

[ Exact Mass ]:
425.11600

[ PSA ]:
59.00000

[ LogP ]:
5.58020

[ Storage condition ]:
2-8℃

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds

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