Small-molecule inhibitor: nafamostat mesilate

Name

History: Nafamostat (as FUT-175) was described as an inhibitor of various serine peptidase, including complement factors, by Fujii et al. (1981).
Peptidases inhibited: A variety of 'trypsin-like' peptidases in family S1 are inhibited. Human tryptase (K_i = 95 pM: Mori et al., 2003). Nafamostat inhibited trypsin, plasmin, thrombin, pancreatic kallikrein, C1r and C1s more potently than did either gabexate mesilate or leupeptin (Ino et al., 1986). Factor D is also inhibited (Inagi et al., 1994). Values of Ki have been given as trypsin (15 nM), thrombin (84 nM), C1r (14 nM) and C1s (38 nM) (Fujii et al., 1981).
Mechanism: Inhibition is reversible.
Pharmaceutical relevance: Nafamostat has been proposed for use as a drug in a variety of conditions including acute pancreatitis (Matsukura et al., 2006) and inflammatory bowel disease (Isozaki et al., 2006). Animal experiments also suggest that it might be useful in inflammatory asthma (Chen et al., 2006).

CID at PubChem: 54953
Structure
Chemical/biochemical name: 6-amidino-2-naphthyl-4-guanidinobenzoate-dimethanesulfonate
Formula weight: 539