144055-55-0
144055-55-0 结构式
常见问题列表
IC50: 83 nM (Human neutrophil elastase), 22 nM (Mouse neutrophil elastase) and 100 nM (Porcine pancreatic elastase);
Ki: 4.2 nM (Human neutrophil elastase)
FK706 effectively inhibits the hydrolysis of bovine neck ligament elastin (2 mg/mL final concentration) by human neutrophil elastase (4 μg/mL final concentration) with an
IC50
value of 230 nM.
FK706 blocks the release of inflammatory chemokines, suppresses the expression of IL-8 and MCP-1 mRNA, and suppresses NF-κB activation. It seems possible that FK706 may directly blocks human lung fibroblasts activation of NF-κB, preventing expression of inflammatory chemokines during cigarette smoke–induced lung inflammation.
FK706 (10-100 mg/kg; subcutaneous injection; for 1-6 hours; male C57BL mice) treatment significantly suppresses human neutrophil elastase (20 μg/paw)-induced paw edema in mice in a dose-dependent manner (47% inhibition at a dose of 100 mg/kg).
| Animal Model: | Male C57BL mice (6 weeks old) injected with human neutrophil elastase |
| Dosage: | 10 mg/kg, 32 mg/kg, 100 mg/kg |
| Administration: | Subcutaneous injection; for 1 hour, 2 hours, 4 hours, 6 hours |
| Result: | Significantly suppressed human neutrophil elastase-induced paw edema in mice in a dose-dependent manner. |