DG051 HCl salt
CAS No. | 929915-58-2 | Cat. No. | BCP16867 |
Name | DG051 HCl salt | ||
Synonyms | DG-051 HCl salt;DG 051 HCl salt; | ||
Formula | C21H25Cl2NO4 | M. Wt | 426.33 |
Description | InVitro: 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 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. | ||
Pathways | Protease/Metabolic Enzyme | ||
Targets | Aminopeptidase |
Structure
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