• Gabexate is a serine protease inhibitor which is used therapeutically (as gabexate mesilate) in the treatment of pancreatitis, disseminated intravascular coagulation, and as a regional anticoagulant for haemodialysis. (wikipedia.org)
  • Gabexate Mesylate is a serine protease inhibitor with IC50 of 0.19 μM which is used therapeutically in the treatment of pancreatitis and disseminated intravascular coagulation. (absource.de)
  • The effects of the cholecystokinin (CCK)-receptor antagonist proglumide, the protease inhibitor gabexate, and the hormones secretin and cholecystokinin-octapeptide (CCK-8) were studied in a model of acute hemorrhagic pancreatitis induced by feeding mice a choline-deficient, ethionine-supplemented (CDE) diet. (duke.edu)
  • Gabexate for the prevention of pancreatic damage related to endoscopic retrograde cholangiopancreatography. (wikipedia.org)
  • Injections of gabexate and proglumide from initiation of CDE diet (before induction of pancreatitis) increased survival from 37% (diet alone) to 85 and 75%, respectively, and also ameliorated histological alterations and increases in serum amylase concentration and pancreatic activated trypsin. (duke.edu)
  • 2) Protease activation in pancreatic acinar cells considered as the early hallmark event in the acute pancreatitis. (uni-greifswald.de)
  • When proglumide or gabexate were given after induction of pancreatitis, proglumide still increased survival to 75%, whereas gabexate no longer did. (duke.edu)
  • Injection of nontoxic doses of CCK-8 before proglumide or gabexate injections completely abolished all beneficial effects and also increased the severity of pancreatitis due to CDE diet alone. (duke.edu)
  • Blockade of CCK receptors and early inhibition of protease activity may be beneficial in severe acute pancreatitis. (duke.edu)
  • It is generally believed that earliest event in acute pancreatitis occur in acinar cells which includes premature protease activation and cytoplasmic vacuole formation. (uni-greifswald.de)
  • Premature trypsinogen activation has been considered as chief culprit as it can activate other proteases in a cascade like manner in acinar cells. (uni-greifswald.de)
  • Activated proteases mediate acinar cell injury and hereby cause the release of chemokines, which in turn attract inflammatory cells. (uni-greifswald.de)
  • A serine protease indicated in Japan to treat chronic pancreatitis. (drugbank.com)
  • However, its entry into the host cells is mediated by transmembrane proteases, of which the transmembrane serine protease 2 (TMPRSS2) is the main one. (encyclopedia.pub)
  • The administration of synthetic protease inhibitors and antifibrinolytic therapy is recommended in patients with the bleeding and massive bleeding types of DIC. (biomedcentral.com)
  • Furthermore, the administration of natural protease inhibitors is recommended in patients with the organ failure type of DIC, while antifibrinolytic treatment is not. (biomedcentral.com)
  • Gabexate mesylate inhibits trypsin, plasmin, plasma kallikrein and thrombin (IC 50 values are 9.4, 30, 41 and 110 μ M respectively). (bio-techne.com)
  • Gabexate mesylate also inhibits LPS-induced TNF- α production, probably by inhibiting NF- κ B and AP-1 activation. (bio-techne.com)
  • Gabexate mesylate attenuates allergen-induced airway inflammation and eosinophils infiltration in the lung of asthma murine model. (bio-techne.com)
  • A direct-acting antiviral agent that inhibits HCV NS3/4A protease to treat chronic hepatitis C virus (HCV) infection in adults with HCV genotype 1 or 4. (drugbank.com)
  • Recent studies have identified several key amino-acidic residues for S-protein interactions with the human ACE2 receptor and the TMPRSS2 membrane protease to initiate infection [ 6 ] . (encyclopedia.pub)
  • Since ACE2 and TMPRSS2 are co-expressed in a limited number of tissues, the high viral transmissibility and the tissue tropism suggest that SARS-CoV-2 may use other proteases for cellular entry [ 7 ] . (encyclopedia.pub)
  • In fact, several proteases have been found to be involved in the transmission or infection process, including furin (a membrane-bound protease expressed in different tissues, mainly in the lungs [ 6 ] ), ADAM17 (short for a disintegrin and metalloprotease 17), and cathepsin L. (encyclopedia.pub)