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Gabexate mesylate Catalog No.GC13711

Trypsin-like serine proteinases inhibitor

Size Price Stock Qty
10mM (in 1mL DMSO)
$47.00
In stock
5mg
$37.00
In stock
50mg
$141.00
In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical Properties

Cas No. 56974-61-9 SDF
Chemical Name ethyl 4-[6-(diaminomethylideneamino)hexanoyloxy]benzoate;methanesulfonic acid
Canonical SMILES CCOC(=O)C1=CC=C(C=C1)OC(=O)CCCCCN=C(N)N.CS(=O)(=O)O
Formula C16H23N3O4.CH4O3S M.Wt 417.48
Solubility ≥18.2 mg/mL in DMSO, ≥99.8 mg/mL in EtOH, ≥102.4 mg/mL in H2O Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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Background

Gabexate mesylate is a non-antigenic synthetic inhibitor of trypsin-like serine proteinases with Ki values of 3.4nM and 180nM, respectively for human tryptase and bovine tryptase [1].

Gabexate mesylate is a drug used in the treatment of pancreatitis, disseminated intravascular coagulation and as a regional anticoagulant for hemodialysis. Gabexate mesylate is reported to bind 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 [1].

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 [2].

References:
[1] Erba F, Fiorucci L, Pascarella S, Menegatti E, Ascenzi P, Ascoli F. Selective inhibition of human mast cell tryptase by gabexate mesylate, an antiproteinase drug. Biochem Pharmacol. 2001 Feb 1;61(3):271-6.
[2] Colasanti M, Persichini T, Venturini G, Menegatti E, Lauro GM, Ascenzi P. Effect of gabexate mesylate (FOY), a drug for serine proteinase-mediated diseases, on the nitric oxide pathway. Biochem Biophys Res Commun. 1998 May 19;246(2):453-6.