DG051

Research use only, not for human use.

A potent, selective LTA4H (Leukotriene A4 hydrolase) inhibitor (IC50/Kd=47/25 nM) of leukotriene B4 biosynthesis.

A potent, selective LTA4H (Leukotriene A4 hydrolase) inhibitor (IC50/Kd=47/25 nM) of leukotriene B4 biosynthesis; dispalys selectivity over a panel of more than 50 targets including aminopeptidases, hERG, GPCRs; has high aqueous solubility (>30 mg/mL) and high oral bioavailability.Heart Failure Phase 2 Discontinued.

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.

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DG-051 | DG 051

Metabolic Enzyme/Protease

Aminopeptidase

Aminopeptidase

Metabolic Disease

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929915-58-2

426.3335

C21H25Cl2NO4

>98% (HPLC)

DMSO: ≥ 325 mg/mL

O=C(O)CCCN1[C@H](COC2=CC=C(OC3=CC=C(Cl)C=C3)C=C2)CCC1.[H]Cl

1-Pyrrolidinebutanoic acid, 2-[[4-(4-chlorophenoxy)phenoxy]methyl]-, hydrochloride (1:1), (2S)-

(-20℃)

With Ice Pack

≥ 2 years