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Fulacimstat

Chemical Structure : Fulacimstat

CAS No.: 1488354-15-9

Fulacimstat (BAY 1142524, BAY1142524, BAY-1142524)

Catalog No.: PC-60514Not For Human Use, Lab Use Only.

Fulacimstat (BAY 1142524, BAY1142524) is a potent, orally available chymase inhibitor with IC50 of 4 nM and 3 nM for human and hamster chymase enzyme, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Fulacimstat (BAY 1142524, BAY1142524) is a potent, orally available chymase inhibitor with IC50 of 4 nM and 3 nM for human and hamster chymase enzyme, respectively.
Fulacimstat (BAY 1142524) blocks the generation of profibrotic chymase-dependent factors such as Ang II, ET-1, and TGF-β1 in vitro with a nanomolar IC50.
Fulacimstat (BAY 1142524) reduces isoprenaline-induced cardiac fibrosis and attenuates the deterioration of heart function after MI, increases left-ventricular ejection fraction in dogs with LVD induced by intracoronary microembolization with no effects on blood pressure or heart rate. 

Physicochemical Properties

M.Wt 487.39
Formula C23H16F3N3O6
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1-(3-methyl-2-oxo-1,3-benzoxazol-6-yl)-2,4-dioxo-3-[(1R)-4-(trifluoromethyl)-2,3-dihydro-1H-inden-1-yl]pyrimidine-5-carboxylic acid

References

1. Kanefendt F, et al. Clin Pharmacol Drug Dev. 2018 Jun 7. doi: 10.1002/cpdd.579.

2. Hanna Tinel, et al. Abstract 13624: A Novel Chymase Inhibitor BAY 1142524 Reduces Fibrosis and Improves Cardiac Function After Myocardial Infarction in Hamster. Circulation. 2017;136:A13624.

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