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- Nafamostat mesylate 82956-11-4

- Nafamostat mesylate 82956-11-4
Nafamostat mesylate 82956-11-4
产品描述 描述 Nafamostat mesilate is a synthetic serine protease inhibitor, used as an anticoagulant during hemodialysis.
纯度 99%储存/保存方法 Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.基本信息 别名 甲磺酸萘莫司他;FUT-175外观 白色至类白色结晶性可溶性/溶解性 DMSO : 54 mg/mL (100 mM)
water : 54 mg/mL (100 mM)l生物活性 靶点 serine proteaseIn vitro(体外研究) Nafamostat mesilate significantly inhibits the release of platelet beta-thromboglobulin (beta TG) at 60 and 120 min. Nafamostat mesilate (NM) prevents any significant release of neutrophil elastase; at 120 min, plasma elastase-alpha 1-antitrypsin complex is 0.16 mg/mL in the NM group and 1.24 mg/mL in the control group. Nafamostat mesilate completely inhibits formation of complexes of C1 inhibitor with kallikrein and FXIIa. Nafamostat mesilate inhibits several proteases which may be importantly involved in the pathophysiology of disseminated intravascular coagulation (DIC).Nafamostat mesilate inhibits extrinsic pathway activity (TF-F.VIIa mediated-F.Xa generation) in a concentration dependent manner with IC50 of 0.1 μM. Nafamostat mesilate produces concentration-dependent inhibition of the initial-phase transient component of biphasic ASIC3 currents with an IC50 value of approximately 2.5 mM.In vivo(体内研究) Nafamostat mesilate (10 mg/kg) inhibits scratching induced by tryptase but not by histamine and serotonin. Nafamostat mesilate (1-10 mg/kg) produces the dose-dependent inhibition of scratching induced by intradermal compound 48/80 (10 mg/site). Nafamostat mesilate (10 mg/kg) suppresses tryptase activity in the mouse skin. Nafamostat mesilate inhibits gemcitabine-induced NF-kappaB activation, enhances apoptosis by gemcitabine and suppresses pancreatic tumor growth. Nafamostat mesilate combined with Gemcitabine improves the body weight loss of mice induced by Gemicitabine.参考文献 参考文献 1. Sundaram S, et al. Thromb Haemost, 1996, 75(1), 76-82.
2. Uchiba M, et al. Thromb Res, 1994, 74(2), 155-161.
研究领域 研究领域 CancerCancer MetabolismCancerTumor immunologyMetabolismTypes of diseaseDrug DiscoverySmall Molecule DrugLead Compound DiscoveryNafamostat mesylate 82956-11-4温馨提示:本产品仅作科研实验使用,不支持临床等研究
