1488354-15-9

1488354-15-9 structure

Name: Fulacimstat
Chemical Name: fulacimstat
CAS Number: 1488354-15-9
Molecular Formula: C₂₃H₁₆F₃N₃O₆
Molecular Weight: 487.385
Catalog: Research Areas Cardiovascular Disease
Create Date: 2019-01-20 02:12:09
Modify Date: 2025-08-24 22:23:39
Fulacimstat is an orally available chymase inhibitor, with IC50s of 4, 3 nM for human and hamster chymase enzyme, respectively.

Name	fulacimstat
Synonyms	VIR72PP4ZU 1-(3-Methyl-2-oxo-2,3-dihydro-1,3-benzoxazol-6-yl)-2,4-dioxo-3-[(1R)-4-(trifluoromethyl)-2,3-dihydro-1H-inden-1-yl]-1,2,3,4-tetrahydro-5-pyrimidinecarboxylic acid fulacimstat 5-Pyrimidinecarboxylic acid, 1-(2,3-dihydro-3-methyl-2-oxo-6-benzoxazolyl)-3-[(1R)-2,3-dihydro-4-(trifluoromethyl)-1H-inden-1-yl]-1,2,3,4-tetrahydro-2,4-dioxo-

Description	Fulacimstat is an orally available chymase inhibitor, with IC50s of 4, 3 nM for human and hamster chymase enzyme, respectively.
Related Catalog	Signaling Pathways >> Others >> Others Research Areas >> Cardiovascular Disease
Target	IC50: 4 nM (human chymase enzyme), 3 nM (hamster chymase enzyme)[1][2].
In Vitro	Fulacimstat inhibits human and hamster chymase enzyme with IC50s of 4 nM and 3 nM, respectively[1][2].
In Vivo	Isoprenaline induces cardiac fibrosis (24.4±1.8%) in hamsters, which is reduced dose dependently by Fulacimstat (16.4±1.2%, 12.4 ± 1.3%, 10.9±1.4% at 1, 3 and 10 mg/kg respectively) and by enalapril (17.7±1.5% at 20 mg/kg). Four weeks after MI, hamster hearts show an increased end diastolic pressure, and reduce contractility and relaxation. Compared to placebo (19.3±2 mmHg), Fulacimstat at 10 mg/kg reduce significantly the end diastolic pressure (13.2±1.4 mmHg) without any effects on blood pressure or heart rate. Moreover, treatment with Fulacimstat reduce the fibrotic area and improve the cardiac response to adrenergic stimulation[1].
References	[1]. Hanna Tinel, et al. Abstract 13624: A Novel Chymase Inhibitor BAY 1142524 Reduces Fibrosis and Improves Cardiac Function After Myocardial Infarction in Hamster. Circulation. 2018;136:A13624. [2]. Kanefendt F, et al. Pharmacokinetics, Safety, and Tolerability of the Novel Chymase Inhibitor BAY 1142524 in Healthy Male Volunteers. Clin Pharmacol Drug Dev. 2018 Jun 7.