ZD-0892

ZD-0892 is a selective and potent inhibitor of a neutrophil elastase with Kis of 6.7 and 200 nM for human neutrophil elastase and porcine pancreatic elastase, respectively.

Signaling Pathways >> Metabolic Enzyme/Protease >> Elastase

Research Areas >> Cardiovascular Disease

Ki: 6.7 nM (Human neutrophil elastase), 200 nM (Human neutrophil elastase)[1]

ZD0892 administration to DBA/2 mice infected with the EMC virus results in reduced myocardial elastolytic activity and coronary microvascular perfusion injury. ZD0892 decreases the pathologic severity of the myocardial lesions associated with murine viral myocarditis[1]. ZD-0892 can reverse advanced pulmonary vascular disease produced in rats[2].

Rats[2] Adult male Sprague-Dawley rats (250-300 g in body weight) are induced pulmonary hypertension. In addition to a group of untreated rats, the experimental groups include rats that receive twice-daily gavage tube feedings of ZD0892, at a dose of 240 mg/kg per day or vehicle (5% polyethylene glycol or dimethyl sulfoxide). Rats are examined after 7 days of treatment. Mice[1] DBA/2 male mice 8 weeks old is used. ZD0892 is given in a dose of 60 mg/kg or 120 mg/kg[1].

[1]. Lee JK, et al. A serine elastase inhibitor reduces inflammation and fibrosis and preserves cardiac function after experimentally-induced murine myocarditis. Nat Med. 1998 Dec;4(12):1383-91.

[2]. Cowan KN, et al. Complete reversal of fatal pulmonary hypertension in rats by a serine elastase inhibitor. Nat Med. 2000 Jun;6(6):698-702.

DMP 777 | GW311616 | Sivelestat Sodium tetrahydrate | Alvelestat | AE-3763 | BAY 678 | BAY-85-8501 | Lodelaben | ZD8321