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Submit ReviewGabexate mesylate is a serine protease inhibitor; Gabexate mesylate inhibits trypsin, plasmin, plasma kallikrein and thrombin (IC50 values are 9.4, 30, 41 and 110 μM respectively). Antithrombotic in vitro and in vivo. Gabexate mesylate also inhibits LPS-induced TNF-α production, probably by inhibiting NF-κB and AP-1 activation. Gabexate mesylate attenuates allergen-induced airway inflammation and eosinophils infiltration in the lung of asthma murine model.
分子量 | 417.48 |
公式 | C16H23N3O4.CH3SO3H |
储存 | Desiccate at RT |
纯度 | ≥98% (HPLC) |
CAS Number | 56974-61-9 |
PubChem ID | 6604915 |
InChI Key | ICDMLAQPOAVWNH-HAAQQRBASA-N |
Smiles | CS(O)(=O)=O.CCOC(=O)C1=CC=C(OC(=O)CCCCCNC(N)=N)C=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 41.75 | 100 |
以下数据基于产品分子量 417.48。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.4 mL | 11.98 mL | 23.95 mL |
5 mM | 0.48 mL | 2.4 mL | 4.79 mL |
10 mM | 0.24 mL | 1.2 mL | 2.4 mL |
50 mM | 0.05 mL | 0.24 mL | 0.48 mL |
参考文献是支持产品生物活性的出版物。
Ohno et al (1980) FOY: [Ethyl p-(6-guanidinohexanoyloxy) benzoate] methanesulfonate as a serine proteinase inhibitor. I. Inhibition of thrombin and factor Xa in vitro. Thromb.Res. 19 579 PMID: 6449757
Ohno et al (1981) FOY: [Ethyl p-(6-guanidinohexanoyloxy) benzoate] methanesulfonate as a serine proteinase inhibitor. II. In vivo effect on coagulo-fibrinolytic system in comparison with he. or apro. Thromb.Res. 24 445 PMID: 6178174
Tamura et al (1977) Synthetic inhibitors of trypsin, plasmin, kallikrein, thrombin, C1r and C1 esterase. Biochim.Biophys.Acta 484 417 PMID: 143965
Yuksel et al (2003) Gabexate mesilate, a synthetic protease inhibitor, inhibits lipopolysaccharide-induced tumor necrosis factor-α production by inhibiting activation of both nuclear factor-κB and activator protein-1 in human monocytes. J.Pharmacol.Exp.Ther. 305 298 PMID: 12649382
Chen et al (2006) Serine protease inhibitors nafamostat mesilate and gabexate mesilate attenuate allergen induced airway inflammation and eosinophilia in a murine model of asthma. J.Allergy Clin.Immunol. 118 105 PMID: 16815145
If you know of a relevant reference for Gabexate mesylate, please let us know.
关键词: Gabexate mesylate, Gabexate mesylate supplier, Serine, protease, inhibits, inhibitors, thrombin, trypsin, kallikrein, plasmin, TNF-α, TNF-alpha, production, antithrombotic, agent, Proteases, Proteinases, Interleukins, Tumor, Necrosis, Factor-α, Factor-alpha, Cytokines, PAR, Receptors, Protease-Activated, proteinase, FOY, Other, 1798, Tocris Bioscience
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