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FK706 is a slow-binding and competitive human neutrophil elastase inhibitor (IC50: 83 nM; Ki: 4.2 nM). FK706 also inhibits mouse neutrophil elastase and porcine pancreatic elastase (IC50s: 22 nM and 100 nM, respectively). FK706 has an anti-inflammatory effect.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | $1,530 | 8-10 weeks | |
50 mg | $1,990 | 8-10 weeks | |
100 mg | $3,190 | 8-10 weeks |
Description | FK706 is a slow-binding and competitive human neutrophil elastase inhibitor (IC50: 83 nM; Ki: 4.2 nM). FK706 also inhibits mouse neutrophil elastase and porcine pancreatic elastase (IC50s: 22 nM and 100 nM, respectively). FK706 has an anti-inflammatory ef |
Targets&IC50 | Pancreatic elastase (porcine):100 nM, Neutrophil elastase (human):(ki)4.2 nM, Neutrophil elastase (human):83 nM, Neutrophil elastase (mouse):22 nM |
In vitro | FK706 effectively inhibits the hydrolysis of bovine neck ligament elastin (2 mg/mL final concentration) by human neutrophil elastase (4 μg/mL final concentration) (IC50: 230 nM) [1]. It blocks the release of inflammatory chemokines, suppresses the expression of IL-8 and MCP-1 mRNA, and inhibits NF-κB activation. FK706 may directly block human lung fibroblasts activation of NF-κB, preventing the expression of inflammatory chemokines during cigarette smoke-induced lung inflammation [2]. |
In vivo | Subcutaneous injection of FK706 (10-100 mg/kg; 1-6 hours; male C57BL mice) significantly inhibits human neutrophil elastase (20 μg/paw)-induced paw edema in a dose-dependent manner (47% inhibition at 100 mg/kg) [1]. |
Molecular Weight | 593.556 |
Formula | C26H33F3N4NaO7 |
Cas No. | 144055-55-0 |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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