FK706

COA

级别和纯度:

≥99%

CAS编号: 144055-55-0
分子式: C₂₆H₃₂F₃N₄NaO₇
分子量: 592.54
PubChem编号: 23690296

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货号 (SKU)	包装规格	是否现货
F651524-5mg	5mg	期货
F651524-10mg	10mg	期货
F651524-25mg	25mg	期货

查看相关系列

Amino Acid/Protein Metabolism (4559) Elastase (31) Metabolic Enzyme/Protease (4889)

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基本描述

规格或纯度	≥99%
英文名称	FK706
生化机理	FK706 是一种强效、缓慢结合的人中性粒细胞弹性蛋白酶竞争性抑制剂，IC 50 为 83 nM，K i 为 4.2 nM。FK706 还能抑制小鼠中性粒细胞弹性蛋白酶和猪胰腺弹性蛋白酶，其 IC 50 s 分别为 22 nM 和 100 nM。
储存温度	2-8°C储存,干燥
运输条件	冰袋运输
作用类型	抑制剂
产品介绍	FK706 is a potent, slow-binding and competitive inhibitor of human neutrophil elastase with an IC 50 of 83 nM and a K i of 4.2 nM. FK706 also inhibits mouse neutrophil elastase and porcine pancreatic elastase with IC 50 s 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 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) 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. Form:Solid IC50& Target:IC50: 83 nM (Human neutrophil elastase), 22 nM (Mouse neutrophil elastase) and 100 nM (Porcine pancreatic elastase), ,Ki: 4.2 nM (Human neutrophil elastase)
纯度	≥99%

名称和识别符

IIUPAC Name	sodium;2-[[4-[[(2S)-3-methyl-1-oxo-1-[(2S)-2-[(1,1,1-trifluoro-4-methyl-2-oxopentan-3-yl)carbamoyl]pyrrolidin-1-yl]butan-2-yl]carbamoyl]benzoyl]amino]acetate
INCHI	1S/C26H33F3N4O7.Na/c1-13(2)19(21(36)26(27,28)29)31-24(39)17-6-5-11-33(17)25(40)20(14(3)4)32-23(38)16-9-7-15(8-10-16)22(37)30-12-18(34)35;/h7-10,13-14,17,19-20H,5-6,11-12H2,1-4H3,(H,30,37)(H,31,39)(H,32,38)(H,34,35);/q;+1/p-1/t17-,19?,20-;/m0./s1
InChi Key	DNTYCMNNMGACPR-JSAITXCESA-M
Smiles	CC(C)C(C(=O)C(F)(F)F)NC(=O)C1CCCN1C(=O)C(C(C)C)NC(=O)C2=CC=C(C=C2)C(=O)NCC(=O)[O-].[Na+]
Isomeric SMILES	CC(C)[C@@H](C(=O)N1CCC[C@H]1C(=O)NC(C(C)C)C(=O)C(F)(F)F)NC(=O)C2=CC=C(C=C2)C(=O)NCC(=O)[O-].[Na+]
PubChem CID	23690296
MeSH Entry Terms	FK 706;FK706;sodium 2-(4-((1-((2-((3,3,3-trifluoro-1-isopropyl-2-oxopropyl)aminocarbonyl)pyrrolidin-1-yl)carbonyl)-2-methylpropyl)aminocarbonyl)benzoylamino)acetate
分子量	592.54

化学和物理性质

溶解性	DMSO : 115 mg/mL (194.08 mM; Need ultrasonic) H2O : ≥ 100 mg/mL (168.76 mM)

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