| Description | BAY-678 is a human neutrophil elastase (HNE; IC50: 20 nM) inhibitor with oral bioactivity, potency and selectivity.BAY-678 is a chemical probe recommended by the Structural Genomics Consortium (SGC). |
| In vitro | BAY-678 是 Structural Genomics Consortium 的化学探针。[2] BAY-678 对MNE的Ki值为700 nM。BAY-678是新型 HN E抑制剂。[1] |
| In vivo | BAY-678在急性肺损伤（ALI）和肺气肿的临床前模型中显示出显着疗效。在大鼠和小鼠的肺动脉高压（PAH）模型中，BAY-678 展示了显著的有益肺血液动力学和血管效应。[2] |
| Target activity | HNE:20 nM, MNE:700 nM(Ki) |
| molecular weight | 400.35 |
| Molecular formula | C20H15F3N4O2 |
| CAS | 675103-36-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 90.0 mg/mL (224.8 mM) Ethanol: 4.3 mg/mL (10.7 mM) |
| References | 1. von Nussbaum F, et al. Freezing the Bioactive Conformation to Boost Potency: The Identification of BAY 85-8501, a Selective and Potent Inhibitor of Human Neutrophil Elastase for Pulmonary Diseases. ChemMedChem. 2015 Jul;10(7):1163-73. 2. von Nussbaum F, et al. Neutrophil elastase inhibitors for the treatment of (cardio)pulmonary diseases: Into clinical testing with pre-adaptive pharmacophores. Bioorg Med Chem Lett. 2015 Oct 15;25(20):4370-81. 3. BAY-678 Selective chemical probe for Human Neutrophil Elastase. |