DG051 (free acid)

DG051 (free acid) is an effective inhibitor of leukotriene A4 hydrolase (LTA4H), with a Kd of 26 nM. It has high water solubility (greater than 30 mg/mL) and high oral bioavailability (over 80% across different species) . DG051 (free acid) can be used in research related to myocardial infarction and stroke[1][2].

Product Specifications

CAS Number

[929916-05-2]

UNSPSC

12352005

Hazard Statement

H302-H315-H319-H335

Target

Aminopeptidase

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/dg051-free-acid.html

Smiles

ClC(C=C1)=CC=C1OC(C=C2)=CC=C2OC[C@H]3N(CCC3)CCCC(O)=O

Molecular Formula

C21H24ClNO4

Molecular Weight

389.87

Precautions

P261-P264-P270-P271-P280-P302+P352-P304+P340-P330-P362+P364-P405-P501

References & Citations

[1]Enache L A, et al. Development of a scalable synthetic process for DG-051B, a First-in-Class inhibitior of LTA4H[J]. Organic Process Research & Development, 2009, 13 (6) : 1177-1184.|[2]Sandanayaka V, et al. Discovery of 4-[ (2 S) -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, 2010, 53 (2) : 573-585.