| Description | Fulacimstat (BAY1142524) (BAY1142524) is a chymase inhibitor, with IC50s of 3, 4 nM for hamster and human chymase enzyme, respectively. |
| In vivo | 异丙肾上腺素在仓鼠体内诱发心脏纤维化（24.4％），而Fulacimstat的剂量依赖性降低了此现象（分别在1, 3 和 10 mg/kg的剂量下降至16.4％, 12.4％, 10.9％）。心肌梗塞（MI）后四周，仓鼠心脏显示出增加的舒张末压和降低的收缩及松弛能力。与安慰剂（19.3±2 mmHg）相比，10 mg/kg的Fulacimstat显著降低了舒张末压（13.2±1.4 mmHg），同时对血压或心率无影响。此外，Fulacimstat治疗减少了纤维化区域并改善了心脏对肾上腺素刺激的反应[1]。 |
| Target activity | Hamster chymase enzyme:3 nM, Chymase:4 nM |
| Synonyms | BAY1142524 |
| molecular weight | 487.38 |
| Molecular formula | C23H16F3N3O6 |
| CAS | 1488354-15-9 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 5 mg/mL (10.26 mM), Sonication is recommended. |
| 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. |