929915-58-2

929915-58-2 structure

Name: DG051
Chemical Name: 4-{(S)-2-(4-(4-chlorophenoxy)phenoxymethyl)pyrrolidin-1-yl}-1-butyric acid hydrochloride
CAS Number: 929915-58-2
Molecular Formula: C₂₁H₂₅Cl₂NO₄
Molecular Weight: 426.33400
Catalog: Signaling Pathways Metabolic Enzyme/Protease Aminopeptidase
Create Date: 2017-02-28 08:22:46
Modify Date: 2024-01-09 16:02:24
DG051 is a potent leukotriene A4 hydrolase inhibitor of leukotriene B4 biosynthesis in the enzyme assay with an IC50=47 nM.

Name	4-{(S)-2-(4-(4-chlorophenoxy)phenoxymethyl)pyrrolidin-1-yl}-1-butyric acid hydrochloride
Synonyms	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

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.

1198149-97-1

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929915-58-2