切换导航

Nafamostat Mesylate(FUT-175)

现货
Catalog No.
A2586
丝氨酸蛋白酶抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL H2O)
¥ 550.00
现货
10mg
¥ 500.00
现货
50mg
¥ 1,500.00
现货

电话: 021-55669583

邮箱: sales@apexbio.cn

全球经销商

Background

Nafamostat mesylate, previously known as FUT-175, is an inhibitor of serine protease that inhibits a variety of serine proteases, including trypsin and several proteases in the coagulation cascade. Although it was originally developed as an inhibitor of complements, Nafamostat mesylate has been widely used for the treatment of inflammation (such as acute pancreatitis) and disseminated intravascular coagulation (DIC). Nafamostat mesylate exhibits extremely potent inhibition against human tryptase as well as tryptase-catalyzed hydrolysis of Boc-Phe-Ser-Arg-MCA with inhibition constant Kivalue of 95.3 pM. Besides its protease-inhibiting activity, nafamostat mesylate, in a recent study, displayed its antimicrobial activity by dose-dependently inhibiting the proliferation of chlamydial in vitro.

Reference

Robert D Inman and Basil Chiu. Nafamostat mesylate, a serine protease inhibitor, demonstrates novel antimicrobial properties and effectiveness in Chlamydia-induced arthritis. Arthritis Rsearch & Therapy 2012, 13:R150

Shuji Mori, Yoshinori Itoh, Ryoko Shinohata, Toshiaki Sendo, Ryozo Oishi and Masahiro Nishibori. Nafamostat mesilate is an extremely potent inhibitor of human tryptase. J Pharmacol Sci 92, 420-423 (2003)

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt539.59
Cas No.82956-11-4
FormulaC19H17N5O2.2CH4O3S
SynonymsNafamostat Mesylate,FUT-175,Futhan
Solubility≥27mg/mL in DMSO, ≥54mg/mL in H2O
Chemical Name(6-carbamimidoylnaphthalen-2-yl) 4-(diaminomethylideneamino)benzoate;methanesulfonic acid
SDFDownload SDF
Canonical SMILESCS(=O)(=O)O.CS(=O)(=O)O.C1=CC(=CC=C1C(=O)OC2=CC3=C(C=C2)C=C(C=C3)C(=N)N)N=C(N)N
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

人类胰腺肿瘤细胞系PANC-1

溶解方法

该化合物在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月

反应条件

3 h,160 μg/mL

实验结果

通过ELISA评估NF-κB活化,统计学结果表明,在PANC-1细胞的核提取物中,联合用药组的NF-κB p65浓度低于oxaliplatin组(p < 0.0001)。与核NF-κB水平类似,Western印迹分析表明联合用药组中的磷酸化IκBα水平显著低于oxaliplatin组(p = 0.037)。换言之,FUT-175通过在体外抑制IκBa磷酸化来抑制oxaliplatin诱导的NF-κB活化。

动物实验 [1]:

动物模型

5周龄雄性裸鼠

剂量

30 μg/g,每周三次,为期六周,腹膜内注射

实验结果

通过将200 μM PBS中的PANC-1细胞(5×10-6个细胞)皮下注射到动物背部的右侧来建立胰腺癌模型。在体内,Oxaliplatin和nafamostatmesilate联合用药组的肿瘤生长显著慢于oxaliplatin组(p < 0.0001)。联合给药组的肿瘤体积显著低于oxaliplatin组(p = 0.048)。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1] Gocho T, Uwagawa T, Furukawa K, et al. Combination chemotherapy of serine protease inhibitor nafamostatmesilate with oxaliplatin targeting NF-κB activation for pancreatic cancer[J]. Cancer letters, 2013, 333(1): 89-95.

生物活性

Description Nafamostat Mesylate 是一种抗凝剂。
靶点 Serine Protease          
IC50            

质量控制

化学结构

Nafamostat Mesylate(FUT-175)

相关生物数据

Nafamostat Mesylate(FUT-175)

相关生物数据

Nafamostat Mesylate(FUT-175)