Nafamostat |
| Catalog No.GC17676 |
Nafamostat is a synthetic serine protease inhibitor.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 81525-10-2
Sample solution is provided at 25 µL, 10mM.
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Nafamostat 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.
| 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. | 81525-10-2 | SDF | |
| Chemical Name | (6-carbamimidoylnaphthalen-2-yl) 4-(diaminomethylideneamino)benzoate | ||
| Canonical SMILES | C1=CC(=CC=C1C(=O)OC2=CC3=C(C=C2)C=C(C=C3)C(=N)N)N=C(N)N | ||
| Formula | C19H17N5O2 | M.Wt | 347.37 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.8788 mL | 14.3939 mL | 28.7877 mL |
| 5 mM | 575.8 μL | 2.8788 mL | 5.7575 mL |
| 10 mM | 287.9 μL | 1.4394 mL | 2.8788 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 29 reference(s) in Google Scholar.)
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