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144055-55-0

中文名稱 FK706
英文名稱 FK 706
CAS 144055-55-0
更新日期 2023/03/20 15:41:21
分子式 C26H34F3N4NaO7
分子量 594.56
MOL 文件 144055-55-0.mol
144055-55-0 結(jié)構(gòu)式 144055-55-0 結(jié)構(gòu)式

基本信息

中文別名
化合物 T15285
英文別名
FK 706

物理化學(xué)性質(zhì)

儲存條件4°C, protect from light
溶解度DMSO: 115 mg/mL (194.08 mM)
形態(tài)Solid
顏色White to off-white

常見問題列表

生物活性
FK706 是一種有效,緩慢結(jié)合和競爭性的人中性粒細(xì)胞彈性蛋白酶抑制劑,IC50 為 83 nM,Ki 為 4.2 nM。FK706 還抑制小鼠中性粒細(xì)胞彈性蛋白酶和豬胰彈性蛋白酶,IC50 分別為 22 nM 和 100 nM,并且對其他絲氨酸蛋白酶 (例如人胰胰蛋白酶,人胰腺α-胰凝乳蛋白酶和人白細(xì)胞組織蛋白酶G) 沒有抑制活性。FK706 具有抗炎作用。
靶點

IC50: 83 nM (Human neutrophil elastase), 22 nM (Mouse neutrophil elastase) and 100 nM (Porcine pancreatic elastase);
Ki: 4.2 nM (Human neutrophil elastase)

體外研究

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.

體內(nèi)研究

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.
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