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Description: Gabexate Mesylate (Megacert; Arodate) is a novel, potent and synthetic inhibitor of serine protease with anti-coagulant activity. It inhibits serine protease with IC50 of 0.19 μM and is used for the treatment of pancreatitis and disseminated intravascular coagulation. Gabexate mesylate binds to the primary specificity site S1 of human and bovine tryptases. The carbonyl group of gabexate mesylate interacts with the oxyanion binding hole of the enzyme. The tighter binding of gabexate mesylate to human tryptase results in a higher affinity than to bovine tryptase.
References: Biochem Biophys Res Commun. 1998 May 19;246(2):453-6.
Chemical Name: 4-[[6-[(Aminoiminomethyl)amino]-1-oxohexyl]oxy]-benzoic acid ethyl ester mesylate
InChi Key: DNTNDFLIKUKKOC-UHFFFAOYSA-N
InChi Code: InChI=1S/C16H23N3O4.CH4O3S/c1-2-22-15(21)12-7-9-13(10-8-12)23-14(20)6-4-3-5-11-19-16(17)18;1-5(2,3)4/h7-10H,2-6,11H2,1H3,(H4,17,18,19);1H3,(H,2,3,4)
SMILES Code: O=C(OCC)C1=CC=C(OC(CCCCCNC(N)=N)=O)C=C1.OS(=O)(C)=O
Megacert; Mesyl Gabexate; gabexate mesilate; Arodate; Megacart; Gabexate; Gabexate mesylate; Arodate.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
In vitro activity: Gabexate mesylate is also found to inhibit cNOS and iNOS, with Ki values of 150μM and 5mM. It up-regulates iNOS gene expression. In addition, gabexate mesylate inhibits the LPS/IFNγ-induced NO production with EC50 value of 250μM
Cell Assay: 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
Biochem Biophys Res Commun. 1998 May 19;246(2):453-6.
Purity ≥98%
COA
MSDS