Gabexate (mesylate)

Gabexate mesylate (FOY) is is a competitive and non-antigenic synthetic inhibitor of trypsin-like serine proteinases. Gabexate mesylate inhibits human thrombin, urokinase, plasmin, and Factor Xa with Kis of 0.97, 1.3, 1.6, and 8.5 μM, respectively. Gabexate mesylate binds to human and bovine tryptase with Kis of 3.4 nM and 18 μM, respectively. Gabexate mesylate exerts an anticoagulant effect on the clotting activity of thrombin and has anti-inflammatory effect by viainhibition of NF-κB, proinflammatory cytokines, and nitric oxide. Gabexate mesylate is used for pancreatitis and disseminated intravascular coagulation[1][2][3][4].

Product Specifications

CAS Number

[56974-61-9]

Product Name Alternative

FOY

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Factor Xa; Proteasome

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/Gabexate-mesylate.html

Concentration

10mM

Purity

98.64

Solubility

DMSO : ≥ 100 mg/mL|H2O : 7.14 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C17H27N3O7S

Molecular Weight

417.48

Precautions

H302, H315, H319, H335

References & Citations

[1]H Ohno, et al. FOY: [ethyl P- (6-guanidinohexanoyloxy) benzoate] methanesulfonate as a serine proteinase inhibitor. I. Inhibition of thrombin and factor Xa in vitro. Thromb Res. 1980;19 (4-5) :579-88.|[2]F Erba, et al. Selective inhibition of human mast cell tryptase by gabexate mesylate, an antiproteinase drug. Biochem Pharmacol. 2001 Feb 1;61 (3) :271-6.|[3]Tsuneo Ozeki, et al. The specific inhibition of HepG2 cells proliferation by apoptosis induced by gabexate mesilate. Int J Clin Exp Pathol. 2010 Aug 15;3 (7) :710-7.|[4]Seon Hee Oh, et al. Gabexate mesilate ameliorates the neuropathic pain in a rat model by inhibition of proinflammatory cytokines and nitric oxide pathway via suppression of nuclear factor-κB. Korean J Pain. 2020 Jan 1;33 (1) :30-39.