DG051

DG051

D651905-5mg

5mg

≥99%

2-8°C储存,干燥

冰袋运输

DG051 is a potent leukotriene A4 hydrolase inhibitor of leukotriene B4 biosynthesis in the enzyme assay with an IC 50 =47 nM. In Vitro DG051 is a potent inhibitor of LTA4H aminopeptidase activity against L-alanine p-nitroanilide (IC 50 =72 nM). DG051 inhibits human whole blood (HWB) with IC 50 of 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 strokeDG-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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:IC50: 47 nM (LTA4H)

DG051 是一种强效的白三烯 A4 水合酶抑制剂，在酶测定中可抑制白三烯 B4 的生物合成，IC 50 =47 nM。

929915-58-2

C21H25Cl2NO4

426.33 g/mol

44818987

C1C[C@H](N(C1)CCCC(=O)O)COC2=CC=C(C=C2)OC3=CC=C(C=C3)Cl.Cl

C1C[C@H](N(C1)CCCC(=O)O)COC2=CC=C(C=C2)OC3=CC=C(C=C3)Cl.Cl

44818987

DMSO : ≥ 325 mg/mL (762.32 mM)

2

5

9

425.116 Da

425.116 Da

59.000 Ų

28

0

447.000

0

2