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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]. |
| Synonyms | 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) |
| Color | White |
| Appearance | solid |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||
| Solubility Information | DMSO: 5 mg/mL (10.26 mM), Sonication is recommended. | ||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.05 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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