Fulacimstat 是可口服的糜酶抑制剂，能够作用于人糜酶(IC50:4 nM)和仓鼠糜酶(IC50:3 nM)。

Fulacimstat (BAY1142524) is a chymase inhibitor, with IC50s of 3, 4 nM for hamster and human chymase enzyme, respectively.

Isoprenaline induces cardiac fibrosis (24.4%) in hamsters, which is reduced dose-dependently by Fulacimstat (16.4%, 12.4%, 10.9% at 1, 3 and 10 mg/kg respectively). Four weeks after MI, hamster hearts show increased end-diastolic pressure and reduce contractility and relaxation. Compared to placebo (19.3±2 mmHg), Fulacimstat at 10 mg/kg reduces significantly the end-diastolic pressure (13.2±1.4 mmHg) without any effects on blood pressure or heart rate. Moreover, treatment with Fulacimstat reduces the fibrotic area and improves the cardiac response to adrenergic stimulation [1].

1488354-15-9

C23H16F3N3O6

487.38

BAY1142524;Fulacimstat

DMSO:5 mg/mL (10.26 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years