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Chemical Structure : Fulacimstat
CAS No.: 1488354-15-9
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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $258 | In stock | |
| 10 mg | $398 | In stock | |
| 25 mg | $588 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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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.
| M.Wt | 487.39 | |
| Formula | C23H16F3N3O6 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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 |
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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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