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Chemical Compound Review

CytoFab     (6-carbamimidoylnaphthalen-2- yl) 4...

Synonyms: Nafamostat, Nafamostatum, CHEMBL273264, SureCN135503, SureCN135504, ...
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Disease relevance of Nafamostat


High impact information on Nafamostat


Chemical compound and disease context of Nafamostat


Biological context of Nafamostat


Anatomical context of Nafamostat


Associations of Nafamostat with other chemical compounds


Gene context of Nafamostat

  • Electrophoretic mobility shift assay (EMSA) revealed that LPS activated nuclear factor-kappaB (NF-kappaB) in RAW264.7 cells and that this activation was suppressed by nafamostat mesilate [28].
  • Our observations suggest that nafamostat mesilate is a candidate agent for various diseases such as ischemia-reperfusion, graft rejection, inflammatory diseases, and autoimmune diseases, in which iNOS and/or NF-kappaB are upregulated [28].
  • We found that nafamostat mesilate elicits IL-12, IL-18, tumor necrosis factor-alpha and interferon-gamma production, and the expression of intercellular adhesion molecules-1, B7.1, B7.2, CD40, and CD40 ligand in human peripheral blood mononuclear cells [29].
  • These results suggest that the stabilization of EGF by NM in culture is an important factor in the expression of its effects, and that EGF induces Cu, Zn-SOD expression by accelerating transcription of the Cu, Zn-SOD gene in cells, resulting in their protection from the effects of superoxide anion radicals [23].
  • CONCLUSIONS: Nafamostat mesilate fails to reduce thrombin formation and neutrophil elastase release, whereas minimal-dose aprotinin inhibits both [17].

Analytical, diagnostic and therapeutic context of Nafamostat

  • Although premedication with two kinds of complement inhibitors, soluble complement receptor type 1 (sCR1) or nafamostat mesylate, resulted in inhibition of the IAR after either a single or a double exposure, the LAR was inhibited after the triple [30].
  • We studied the use of depolymerized holothurian glycosaminoglycan (DHG) as an anticoagulant in experimental beagle-dog hemodialysis using a hollow-fiber dialyzer compared to that using unfractionated heparin (UFH), low-molecular-weight heparin (LMWH), and nafamostat mesilate (FUT) [31].
  • Furthermore, we used nafamostat mesilate for coagulopathy prophylaxis during cardiopulmonary bypass [32].
  • The patients were divided into a control group (n = 10) and a nafamostat group (n = 10) [33].
  • Only intra-arterial infusion of nafamostat significantly diminished capillary peritoneal leakage (Evans blue dye, 3.6 +/- 0.9 vs 9.4 +/- 0.4; P <.01) [12].


  1. Hyperkalemia due to nafamostat mesylate. Kitagawa, H., Chang, H., Fujita, T. N. Engl. J. Med. (1995) [Pubmed]
  2. Effectiveness of nafamostat mesilate on glomerulonephritis in immune-complex diseases. Miyata, T., Fujita, Y., Inagi, R., Inoue, I., Sugiyama, S., Maeda, K. Lancet (1993) [Pubmed]
  3. Serine protease inhibitors nafamostat mesilate and gabexate mesilate attenuate allergen-induced airway inflammation and eosinophilia in a murine model of asthma. Chen, C.L., Wang, S.D., Zeng, Z.Y., Lin, K.J., Kao, S.T., Tani, T., Yu, C.K., Wang, J.Y. J. Allergy Clin. Immunol. (2006) [Pubmed]
  4. Effects of protease inhibitors on replication of various myxoviruses. Hosoya, M., Matsuyama, S., Baba, M., Suzuki, H., Shigeta, S. Antimicrob. Agents Chemother. (1992) [Pubmed]
  5. Depolymerized holothurian glycosaminoglycan (DHG), a novel alternative anticoagulant for hemodialysis, is safe and effective in a dog renal failure model. Minamiguchi, K., Kitazato, K.T., Nagase, H., Sasaki, E., Ohwada, K., Kitazato, K. Kidney Int. (2003) [Pubmed]
  6. Nafamostat mesilate reduces blood loss during open heart surgery. Murase, M., Usui, A., Tomita, Y., Maeda, M., Koyama, T., Abe, T. Circulation (1993) [Pubmed]
  7. Involvement of neutrophil recruitment and protease-activated receptor 2 activation in the induction of IL-18 in mice. Ikawa, K., Nishioka, T., Yu, Z., Sugawara, Y., Kawagoe, J., Takizawa, T., Primo, V., Nikolic, B., Kuroishi, T., Sasano, T., Shimauchi, H., Takada, H., Endo, Y., Sugawara, S. J. Leukoc. Biol. (2005) [Pubmed]
  8. Inhibitory effect of serine protease inhibitors on neutrophil-mediated endothelial cell injury. Nakatani, K., Takeshita, S., Tsujimoto, H., Kawamura, Y., Sekine, I. J. Leukoc. Biol. (2001) [Pubmed]
  9. Can nafamostat mesilate be used for temporary management of hemodialysis in a patient with heparin-induced thrombocytopenia (HIT)? Matsuo, T., Matsuo, M., Ouga-Maruyama, S. Thromb. Haemost. (2001) [Pubmed]
  10. Review article: anti-tryptase therapy in inflammatory bowel disease. Yoshida, N., Isozaki, Y., Takagi, T., Takenaka, S., Uchikawa, R., Arizono, N., Yoshikawa, T., Okanoue, T. Aliment. Pharmacol. Ther. (2006) [Pubmed]
  11. Continuous regional arterial infusion of protease inhibitor and antibiotics in acute necrotizing pancreatitis. Takeda, K., Matsuno, S., Sunamura, M., Kakugawa, Y. Am. J. Surg. (1996) [Pubmed]
  12. Regional effects of nafamostat, a novel potent protease and complement inhibitor, on severe necrotizing pancreatitis. Keck, T., Balcom, J.H., Antoniu, B.A., Lewandrowski, K., Warshaw, A.L., Fernández-del Castillo, C.F. Surgery (2001) [Pubmed]
  13. The effects of nafamostat mesilate (FUT-175) on caerulein-induced acute pancreatitis in the rat. Wisner, J.R., Ozawa, S., Renner, I.G. Int. J. Pancreatol. (1989) [Pubmed]
  14. Cardiac tamponade secondary to hemorrhagic pericarditis during continuous hemofiltration for renal failure. The role of the anticoagulant. Hiraide, A., Tazaki, O., Fujii, N., Yoshioka, T., Sugimoto, T. Renal failure. (1994) [Pubmed]
  15. The influence of a serine protease inhibitor, nafamostat mesilate, on plasma coagulation, and platelet activation during experimental Extracorporeal Life Support (ECLS). Mellgren, K., Skogby, M., Friberg, L.G., Tengborn, L., Wadenvik, H. Thromb. Haemost. (1998) [Pubmed]
  16. Effect of nafamostat mesilate on coagulation and fibrinolysis in hepatic resection. Shimada, M., Matsumata, T., Shirabe, K., Kamakura, T., Taketomi, A., Sugimachi, K. J. Am. Coll. Surg. (1994) [Pubmed]
  17. Effects of nafamostat mesilate and minimal-dose aprotinin on blood-foreign surface interactions in cardiopulmonary bypass. Kaminishi, Y., Hiramatsu, Y., Watanabe, Y., Yoshimura, Y., Sakakibara, Y. Ann. Thorac. Surg. (2004) [Pubmed]
  18. Protective effect of nafamostat mesilate in early wound healing. Tsutamoto, Y., Tani, T., Eguchi, Y., Araki, H., Kodama, M. J. Am. Coll. Surg. (1997) [Pubmed]
  19. Serine proteases are involved in the pathogenesis of trauma-hemorrhagic shock-induced gut and lung injury. Deitch, E.A., Shi, H.P., Lu, Q., Feketeova, E., Xu, d.a. .Z. Shock (2003) [Pubmed]
  20. Nafamostat mesilate, a broad spectrum protease inhibitor, modulates platelet, neutrophil and contact activation in simulated extracorporeal circulation. Sundaram, S., Gikakis, N., Hack, C.E., Niewiarowski, S., Edmunds, L.H., Koneti Rao, A., Sun, L., Cooper, S.L., Colman, R.W. Thromb. Haemost. (1996) [Pubmed]
  21. Elimination of Kupffer cells and nafamostat mesilate rinse prevent reperfusion injury in liver grafts from agonal non-heart-beating donors. Tsukamoto, S., Ohkohchi, N., Fukumori, T., Orii, T., Asakura, T., Takayama, J., Shibuya, H., Kato, H., Satomi, S. Transplantation (1999) [Pubmed]
  22. Role of locally formed angiotensin II and bradykinin in the reduction of myocardial infarct size in dogs. Noda, K., Sasaguri, M., Ideishi, M., Ikeda, M., Arakawa, K. Cardiovasc. Res. (1993) [Pubmed]
  23. Effect of epidermal growth factor on Cu, Zn-superoxide dismutase expression in cultured fibroblasts from rat skin. Nishiguchi, K., Kiyohara, Y., Komada, F., Iwakawa, S., Okumura, K. Pharm. Res. (1994) [Pubmed]
  24. Increased tissue factor pathway inhibitor levels in uremic patients on regular hemodialysis. Kario, K., Matsuo, T., Yamada, T., Matsuo, M. Thromb. Haemost. (1994) [Pubmed]
  25. Detection of intermediary Clr with complete active site, using a synthetic proteinase inhibitor. Niinobe, M., Ueno, Y., Hitomi, Y., Fujii, S. FEBS Lett. (1984) [Pubmed]
  26. A potent tryptase inhibitor nafamostat mesilate dramatically suppressed pulmonary dysfunction induced in rats by a radiographic contrast medium. Sendo, T., Itoh, Y., Goromaru, T., Sumimura, T., Saito, M., Aki, K., Yano, T., Oishi, R. Br. J. Pharmacol. (2003) [Pubmed]
  27. Enhanced bioavailability of subcutaneously injected insulin by pretreatment with ointment containing protease inhibitors. Takeyama, M., Ishida, T., Kokubu, N., Komada, F., Iwakawa, S., Okumura, K., Hori, R. Pharm. Res. (1991) [Pubmed]
  28. Nafamostat mesilate suppresses NF-kappaB activation and NO overproduction in LPS-treated macrophages. Noguchi, S., Nakatsuka, M., Konishi, H., Kamada, Y., Chekir, C., Kudo, T. Int. Immunopharmacol. (2003) [Pubmed]
  29. Nafamostat mesilate induces production of interleukin-12 and -18 in human peripheral blood mononuclear cells. Katsuno, G., Takahashi, H.K., Iwagaki, H., Mizuno, K., Mori, S., Yoshino, T., Nishibori, M., Tanaka, N. J. Pharmacol. Sci. (2005) [Pubmed]
  30. Contribution of anaphylatoxin C5a to late airway responses after repeated exposure of antigen to allergic rats. Abe, M., Shibata, K., Akatsu, H., Shimizu, N., Sakata, N., Katsuragi, T., Okada, H. J. Immunol. (2001) [Pubmed]
  31. The anticoagulant and hemorrhagic effects of DHG, a new depolymerized holothurian glycosaminoglycan, on experimental hemodialysis in dogs. Minamiguchi, K., Kitazato, K.T., Sasaki, E., Nagase, H., Kitazato, K. Thromb. Haemost. (1997) [Pubmed]
  32. Nafamostat mesilate treatment during open heart operation in immune thrombocytopenic purpura. Nakamura, K., Onitsuka, T., Yano, M., Nagahama, H., Nakamura, E., Matsuzaki, Y. Ann. Thorac. Surg. (2000) [Pubmed]
  33. Attenuation of cardiopulmonary bypass-derived inflammatory reactions reduces myocardial reperfusion injury in cardiac operations. Sawa, Y., Shimazaki, Y., Kadoba, K., Masai, T., Fukuda, H., Ohata, T., Taniguchi, K., Matsuda, H. J. Thorac. Cardiovasc. Surg. (1996) [Pubmed]
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