Nafamostat mesylate

CAS号

82956-11-4

分子式

C19H17N5O2·2CH4O3S

主要靶点

Serine/threonin kinase|Apoptosis|SARS-CoV|Serine Protease

仅限科研使用

Cat No : CM00390

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Synonyms

甲磺酸萘莫司他|SARS coronavirus|SARSCoV|SARS-CoV|Serine proteases|Serinekinase|SerineProtease|Ser/Thr Protease|Serine endopeptidases|Serine kinase|Serine Protease|threoninkinase|Threonine proteases|threonin kinase|Inhibitor|inhibit|Nafamostat|Nafamostat mesylate|Nafamostat Mesylate|FUT 175|FUT175|FUT-175|Apoptosis



产品信息

CAS号 82956-11-4
分子式 C19H17N5O2·2CH4O3S
主要靶点 Serine/threonin kinase|Apoptosis|SARS-CoV|Serine Protease
主要通路 凋亡|蛋白酶体|微生物学
分子量 539.58
纯度 99.76%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 甲磺酸萘莫司他|SARS coronavirus|SARSCoV|SARS-CoV|Serine proteases|Serinekinase|SerineProtease|Ser/Thr Protease|Serine endopeptidases|Serine kinase|Serine Protease|threoninkinase|Threonine proteases|threonin kinase|Inhibitor|inhibit|Nafamostat|Nafamostat mesylate|Nafamostat Mesylate|FUT 175|FUT175|FUT-175|Apoptosis

体内活性

Nafamostat mesilate能够明显抑制血小板β-血栓球蛋白(βTG)的释放,嗜中性粒细胞弹性蛋白酶的释放,还能够抑制C1抑制剂与激肽释放酶和FXIIa的复合物的形成。Nafamostat mesilate能够抑制TF-F.VIIa介导的F.Xa产生的外源性途径活性(IC50=0.1 μM)。

体外活性

Nafamostat Mesylate抑制gemcitabine诱导的NF-κB活化和细胞凋亡,并抑制胰腺肿瘤的生长.对于胰蛋白酶诱导的划伤,Nafamostat Mesylate(10 mg/kg)能够产生抑制作用.在小鼠皮肤中,Nafamostat Mesylate(10 mg/kg)抑制类胰蛋白酶活性.

溶解度

DMSO:45 mg/mL (83.4 mM);H2O:54 mg/mL (100.08 mM)

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.
3.Ugawa S, et al. Biochem Biophys Res Commun, 2007, 363(1), 203-208.
4.Ui H, et al. Eur J Pharmacol, 2006, 530(1-2), 172-178.
5.Uwagawa T, et al. Anticancer Res, 2009, 29(8), 3173-3178.
6.Homma S, et al. Nafamostat mesilate, a serine protease inhibitor, suppresses interferon-gamma-induced up-regulation of programmed cell death ligand 1 in human cancer cells. Int Immunopharmacol. 2018 Jan;54:39-45.

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