Nafamostat Mesylate(FUT-175)
(Synonyms: 甲磺酸萘莫司他; FUT-175) 目录号 : GC10613
Nafamostat Mesylate(FUT-175)是一种合成的丝氨酸蛋白酶抑制剂。
Cas No.:82956-11-4
Sample solution is provided at 25 µL, 10mM.
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Nafamostat Mesylate(FUT-175) is a synthetic serine protease inhibitor [1]. Nafamostat Mesylate reduces inflammatory responses by inhibiting the complement system, reducing cytokine release, and preventing pancreatic enzyme activation [2]. Nafamostat Mesylate is commonly used to treat acute pancreatitis [3-4].
In SW620 cells, Nafamostat Mesylate (80μg/mL; 3h) prevents NF-κB activation and induces apoptosis in irradiated colorectal cancer cells [5]. In MSTO-211H cells, cell viability was significantly reduced after Nafamostat Mesilate (10μM; 48h) treatment [6]. In YCU-L891 and YCU-H891 cells, Nafamostat Mesylate (10μM; 48h) inhibited the proliferation of two HNSCC cell lines [7].
In choline deficient ethionine diet mice model, Nafamostat Mesylate (20mg/kg; ip; 5d) inhibited the redistribution of cathepsin B activity and the activation of trypsinogen [8]. In xenograft pancreatic cancer mice model, Nafamostat Mesylate (30μg/g; ip; 6 weeks) enhances oxaliplatin-induced tumor growth inhibition [9].
References:
[1]. Mellgren K, Skogby M, Friberg L G, et al. The influence of a serine protease inhibitor, nafamostat mesilate, on plasma coagulation, and platelet activation during experimental extracorporeal life support (ECLS)[J]. Thrombosis and haemostasis, 1998, 79(02): 342-347.
[2]. He Q, Wei Y, Qian Y, et al. Pathophysiological dynamics in the contact, coagulation, and complement systems during sepsis: Potential targets for nafamostat mesilate[J]. Journal of intensive medicine, 2024, 4(04): 453-467.
[3]. Wisner J R, Ozawa S, Renner I G. The effects of nafamostat mesilate (FUT-175) on caerulein-induced acute pancreatitis in the rat[J]. International journal of pancreatology, 1989, 4(4): 383-390.
[4]. Keck T, Balcom J H, Antoniu B A, et al. Regional effects of nafamostat, a novel potent protease and complement inhibitor, on severe necrotizing pancreatitis[J]. Surgery, 2001, 130(2): 175-181.
[5]. Sugano H, Shirai Y, Horiuchi T, et al. Nafamostat mesilate enhances the radiosensitivity and reduces the radiation-induced invasive ability of colorectal cancer cells[J]. Cancers, 2018, 10(10): 386.
[6]. Sutoh T, Fukuda I, Kimura D, et al. Nafamostat mesilate (FUT-175) inhibits cell growth and invasion of malignant pleural mesothelioma cell line, MSTO-211H[J]. Hirosaki Medical Journal, 2010, 61(1): 19-25.
[7]. Yamashita Y, Ishiguro Y, Sano D, et al. Antitumor effects of Nafamostat mesilate on head and neck squamous cell carcinoma[J]. Auris Nasus Larynx, 2007, 34(4): 487-491.
[8]. Hirano T, Takeuchi S. A New Protease Inhibitor, Nafamostat Mesilate (FUT-175), Protects Pancreatic Acinar Cells in CDE-Diet-lnduced Pancreatitis in Mice[J]. Digestive surgery, 1993, 10(4): 182-188.
[9]. Gocho T, Uwagawa T, Furukawa K, et al. Combination chemotherapy of serine protease inhibitor nafamostat mesilate with oxaliplatin targeting NF-κB activation for pancreatic cancer[J]. Cancer Letters, 2013, 333(1): 89-95.
Nafamostat Mesylate(FUT-175)是一种合成的丝氨酸蛋白酶抑制剂 [1]。Nafamostat Mesylate通过抑制补体系统、减少细胞因子释放和阻止胰腺酶活化来减轻炎症反应 [2]。Nafamostat Mesylate常用于治疗急性胰腺炎 [3-4]。
在 SW620 细胞中，Nafamostat Mesylate（80μg/mL；3h）可抑制NF-κB活化并诱导受照射的结直肠癌细胞凋亡 [5]。在MSTO-211H细胞中，Nafamostat Mesylate（10μM；48h）处理后细胞活力显著降低 [6]。在YCU-L891和YCU-H891细胞中，Nafamostat Mesylate（10μM；48h）抑制了两种HNSCC细胞系的增殖 [7]。
在胆碱缺乏的乙硫氨酸饮食小鼠模型中，Nafamostat Mesylate（20mg/kg；ip；5d）抑制了组织蛋白酶B活性的重新分布和胰蛋白酶原的活化 [8]。在异种移植胰腺癌小鼠模型中，Nafamostat Mesylate（30μg/g；ip；6周)增强了奥沙利铂诱导的肿瘤生长抑制作用 [9]。
| Cell experiment [1]: | |
Cell lines | SW620 cells |
Preparation Method | CRC cells were treated with Nafamostat Mesylate (80μg/mL; Nafamostat Mesylate group), ionizing radiation (ionizing radiation group, IR), both Nafamostat Mesylate (80μg/mL) and ionizing radiation (combination group, IR + Nafamostat Mesylate), or vehicle-only (control group, CTR) for the appropriate time. Cells of the IR and combination groups received 2 or 5Gy IR for the cell proliferation assay, and 5Gy IR for the other analyses. In the combination group, the cells were treated with nafamostat mesilate for three hours before IR. |
Reaction Conditions | 80μg/mL; 3h |
Applications | Nafamostat Mesylate prevents NF-κB activation and induces apoptosis in irradiated colorectal cancer cells. |
| Animal experiment [2]: | |
Animal models | Choline deficient ethionine diet mice model |
Preparation Method | Two hundred and sixty young female CD-I mice weighing 12-14g were used. They were allowed an ordinary pellet diet and tap water ad libitum prior to the experiments. After an initial 24-hour fast, they were fed a cholinedeficient diet enriched with 0.5% DZ.-ethionine for 24h. They were again fasted for 24h, then fed a regular laboratory diet and tap water ad libitum for the following 3 days. Up to 20 mice were kept in each cage. All the mice fed the choline deficient ethionine (CDE) diet were then divided into the following two groups: (a) control animals (CDE group) - only 0.2mL of saline was injected subcutaneously; (b) Nafamostat Mesylate-treated animals (Nafamostat Mesylate group) - after the beginning of the CDE diet, Nafamostat Mesylate was injected subcutaneously at a dose of 20mg/kg in 0.2mL of saline. In addition to these two groups, normal mice were also used as a pure control group. |
Dosage form | 20mg/kg; ip; 5d |
Applications | Nafamostat Mesylate inhibited the redistribution of cathepsin B activity and the activation of trypsinogen. |
References: | |
| Cas No. | 82956-11-4 | SDF | |
| 别名 | 甲磺酸萘莫司他; FUT-175 | ||
| 化学名 | (6-carbamimidoylnaphthalen-2-yl) 4-(diaminomethylideneamino)benzoate;methanesulfonic acid | ||
| Canonical SMILES | CS(=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 | ||
| 分子式 | C19H17N5O2.2CH4O3S | 分子量 | 539.59 |
| 溶解度 | ≥ 27mg/mL in DMSO, ≥ 54mg/mL in Water | 储存条件 | 4°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8533 mL | 9.2663 mL | 18.5326 mL |
| 5 mM | 0.3707 mL | 1.8533 mL | 3.7065 mL |
| 10 mM | 0.1853 mL | 0.9266 mL | 1.8533 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00%
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