FK706
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- CAS号:
- 144055-55-0
- 英文名:
- FK 706
- 英文别名:
- FK 706;FK-706,FK706
- 中文名:
- FK706
- 中文别名:
- 化合物 T15285
- CBNumber:
- CB91370798
- 分子式:
- C26H34F3N4NaO7
- 分子量:
- 594.56
- MOL File:
- 144055-55-0.mol
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FK706化学性质
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储存条件:
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4°C, protect from light
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溶解度:
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DMSO: 115 mg/mL (194.08 mM)
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FK706性质、用途与生产工艺
FK706 是一种有效，缓慢结合和竞争性的人中性粒细胞弹性蛋白酶抑制剂，IC50 为 83 nM，Ki 为 4.2 nM。FK706 还抑制小鼠中性粒细胞弹性蛋白酶和猪胰弹性蛋白酶，IC50 分别为 22 nM 和 100 nM，并且对其他丝氨酸蛋白酶 (例如人胰胰蛋白酶，人胰腺α-胰凝乳蛋白酶和人白细胞组织蛋白酶G) 没有抑制活性。FK706 具有抗炎作用。
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).
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Animal Model:
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Male C57BL mice (6 weeks old) injected with human neutrophil elastase
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Dosage:
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10 mg/kg, 32 mg/kg, 100 mg/kg
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Administration:
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Subcutaneous injection; for 1 hour, 2 hours, 4 hours, 6 hours
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Result:
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Significantly suppressed human neutrophil elastase-induced paw edema in mice in a dose-dependent manner.
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FK706
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下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-19269 | FK706 | | 1 mg | 2136元 |
| 2024/04/30 | HY-19269 | FK706
FK706 | 144055-55-0 | 10mg | 7500元 |
144055-55-0, FK706 相关搜索:
- 化合物 T15285
- 144055-55-0
- FK-706,FK706
- FK 706