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FK706 Sale

目录号 : GC61744

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83nM,Ki为4.2nM。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22nM和100nM,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。

FK706 Chemical Structure

Cas No.:144055-55-0

规格 价格 库存 购买数量
5 mg
¥3,971.00
现货
10 mg
¥6,750.00
现货
25 mg
¥13,500.00
现货

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Sample solution is provided at 25 µL, 10mM.

Description

FK706 is a potent, slow-binding and competitive inhibitor of human neutrophil elastase with an IC50 of 83 nM and a Ki of 4.2 nM. FK706 also inhibits mouse neutrophil elastase and porcine pancreatic elastase with IC50s of 22 nM and 100 nM, respectively, and has no inhibitory activity against other serine proteinases such as human pancreatic trypsin, human pancreatic α-chymotrypsin and human leukocyte cathepsin G. FK706 has anti-inflammatory effect[1][2].

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[1]. 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[2].

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)[1]. Animal Model: Male C57BL mice (6 weeks old) injected with human neutrophil elastase[1]

[1]. Shinguh Y, et al. Biochemical and pharmacological characterization of FK706, a novel elastase inhibitor. Eur J Pharmacol. 1997 Oct 15;337(1):63-71. [2]. Numanami H, et al. Serine protease inhibitors modulate smoke-induced chemokine release from human lung fibroblasts. Am J Respir Cell Mol Biol. 2003 Nov;29(5):613-9.

化学性质

Cas No. 144055-55-0 SDF
Canonical SMILES O=C(NC(C(C)C)C(C(F)(F)F)=O)[C@H]1N(C([C@H](C(C)C)NC(C2=CC=C(C(NCC(O[Na])=O)=O)C=C2)=O)=O)CCC1
分子式 C26H32F3N4NaO7 分子量 592.54
溶解度 DMSO: 115 mg/mL (194.08 mM) 储存条件 4°C, protect from light
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1 mg 5 mg 10 mg
1 mM 1.6876 mL 8.4382 mL 16.8765 mL
5 mM 0.3375 mL 1.6876 mL 3.3753 mL
10 mM 0.1688 mL 0.8438 mL 1.6876 mL
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