Gabexate mesylate  (Synonyms: FOY)

Gabexate mesylate is a Factor X inhibitor; serine protease inhibitor . Target: Factor X Gabexate mesylate is a non-antigenic synthetic inhibitor of trypsin-like serine proteinases that is therapeutically used in the treatment of pancreatitis and disseminated intravascular coagulation and as a regional anticoagulant for hemodialysis. Values of the inhibition constant (K(i)) for gabexate mesylate binding to human and bovine tryptase were 3.4 x 10(-9) M and 1.8 x 10(-7) M (at pH 7.4 and 37.0 degrees ), respectively. Gabexate mesylate inhibited the fibrinogenolytic activity of human tryptase [1]. Gabexate Mesylate decreased the TNFalpha production of LPS-stimulated monocytes as shown by the inhibition of mRNA expression and increased the IL-10 production of LPS-stimulated monocytes. Gabexate Mesylate also suppressed the NFkappaB activity of LPS-stimulated monocytes. Inhibitory effect of Gabexate Mesylate on the TNFalpha production of activated human monocytes is mediated by the suppression of NFkappaB activation [2]. Gabexate mesylate inhibits competitively constitutive and inducible NO synthase (cNOS and iNOS, respectively), with Kivalues of 1.0×10 4M and 5.0×10 3M, respectively, at pH 7.4 and 37.0°C. gabexate mesylate increases iNOS mRNA expression in rat C6 glioma cells, as induced byE. colilipopolysaccharide plus interferon-γ. Gabexate mesylate inhibits dose-dependently nitrite production (i.e. NO release) in rat C6 glioma cells, as induced byE. colilipopolysaccharide plus interferon-γ [3].

417.48

Solid

C₁₇H₂₇N₃O₇S

56974-61-9

O=C(OCC)C1=CC=C(OC(CCCCCNC(N)=N)=O)C=C1.CS(=O)(O)=O

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [1]. Erba, F., et al., Selective inhibition of human mast cell tryptase by gabexate mesylate, an antiproteinase drug. Biochem Pharmacol, 2001. 61(3): p. 271-6.  [Content Brief]

  [2]. Aosasa, S., et al., Mechanism of the inhibitory effect of protease inhibitor on tumor necrosis factor alpha production of monocytes. Shock, 2001. 15(2): p. 101-5.  [Content Brief]

  [3]. Colasanti, M., et al., Effect of gabexate mesylate (FOY), a drug for serine proteinase-mediated diseases, on the nitric oxide pathway. Biochem Biophys Res Commun, 1998. 246(2): p. 453-6.  [Content Brief]