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Fulacimstat (BAY1142524) (BAY1142524) is a chymase inhibitor, with IC50s of 3, 4 nM for hamster and human chymase enzyme, respectively.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $108 | In Stock | |
5 mg | $239 | In Stock | |
10 mg | $347 | In Stock | |
25 mg | $569 | In Stock | |
50 mg | $818 | In Stock | |
100 mg | $1,080 | In Stock | |
1 mL x 10 mM (in DMSO) | $256 | In Stock |
Description | Fulacimstat (BAY1142524) (BAY1142524) is a chymase inhibitor, with IC50s of 3, 4 nM for hamster and human chymase enzyme, respectively. |
Targets&IC50 | Hamster chymase enzyme:3 nM, Chymase:4 nM |
In vivo | 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]. |
Alias | BAY1142524 |
Molecular Weight | 487.38 |
Formula | C23H16F3N3O6 |
Cas No. | 1488354-15-9 |
Smiles | Cn1c2ccc(cc2oc1=O)-n1cc(C(O)=O)c(=O)n([C@@H]2CCc3c2cccc3C(F)(F)F)c1=O |
Relative Density. | 1.610 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
Solubility Information | DMSO: 5 mg/mL (10.26 mM), Sonication is recommended. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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