DG051 is a potentleukotriene A4 hydrolaseinhibitor of leukotriene B4 biosynthesis in the enzyme assay with anIC₅₀=47 nM.

IC50: 47 nM (LTA4H)^[1]

DG051 is a potent inhibitor of LTA4H aminopeptidase activity against L-alanine p-nitroanilide (IC₅₀=72 nM). DG051 inhibits human whole blood (HWB) with IC₅₀of 37 nM. As applied within the context of LTA4H inhibitor design, the chemistry team is able to design a potent DG051(K_d=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].

426.33

Solid

C₂₁H₂₅Cl₂NO₄

929915-58-2

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

DMSO : ≥ 325 mg/mL(762.32 mM)

*"≥" means soluble, but saturation unknown.

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。