FK706
目录号 : GC61744FK706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。
Cas No.:144055-55-0
Sample solution is provided at 25 µL, 10mM.
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.
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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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
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 |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >99.50%
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