Fulacimstat

Fulacimstat is an inhibitor of chymase (IC₅₀s = 4 and 3 nM for the human and hamster enzyme, respectively).¹ 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.²

WARNING This product is not for human or veterinary use.

1. Tinel, H., Zubov, D., Zimmermann, K., et al. Abstract 13624: A novel chymase inhibitor BAY 1142524 reduces fibrosis and improves cardiac function after myocardial infarction in hamster. Circulation 136(suppl. 1), A13624 (2017).

2. Sabbah, H.N., Gupta, R.C., and Tinel, H. Abstract 11585: Long-term therapy with a chymase-1 inhibitor (BAY 1142524) improves left ventricular systolic function and prevents progressive chamber remodeling in dogs with heart failure. Circulation 136(suppl. 1), A11585 (2017).