产品描述:
Fulacimstat is an inhibitor of chymase (IC50s = 4 and 3 nM for the human and hamster enzyme, respectively).{66530} It reduces cardiac fibrosis induced by the β1-adrenergic receptor (B1-AR) and β2-AR agonist isoprenaline (isoproterenol; Item No. 15592) in hamsters when administered at doses of 1, 3, and 10 mg/kg. Fulacimstat (2 and 5 mg/kg per day) inhibits microembolism-induced decreases in left ventricular ejection fraction and increases in left ventricular end-systolic volume, decreases in plasma levels of N-terminal pro-brain natriuretic peptide (nt-proBNP), TGF-β1, and TNF-α, as well as the levels of interstitial fibrosis and the cross-sectional area of myocytes, a measure of myocyte hypertrophy, in a coronary microembolism-induced canine model of heart failure.{66531}