Gabexate mesylate - CAS 56974-61-9
Category: Inhibitor
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Molecular Formula:
C17H27N3O7S
Molecular Weight:
417.48
COA:
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Targets:
Factor Xa | Ser/Thr Protease
Description:
Gabexate is a serine protease inhibitor that inhibits trypsin (IC50= 9.4μM), plasmin (IC50= 30μM), plasma kallikrein (IC50= 41μM) and thrombin (IC50= 110μM). It is used therapeutically (as gabexate mesilate) in the treatment of pancreatitis, disseminated intravascular coagulation, and as a regional anticoagulant for haemodialysis.
Appearance:
Solid powder
Synonyms:
4-[[6-[(Aminoiminomethyl)amino]-1-oxohexyl]oxy]-benzoic acid ethyl ester mesylate; Gabexate; Gabexate mesylate; gabexate mesilate. Arodate; Megacart; Megacert; Mesyl Gabexate; Arodate.
Storage:
Store in a cool and dry place (or refer to the Certificate of Analysis).
MSDS:
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InChIKey:
DNTNDFLIKUKKOC-UHFFFAOYSA-N
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)
Canonical SMILES:
O=C(OCC)C1=CC=C(OC(CCCCCNC(N)=N)=O)C=C1.OS(=O)(C)=O
1.A novel thermosensitive in-situ gel of gabexate mesilate for treatment of traumatic pancreatitis: An experimental study.
Gao HJ1,2, Song Q3, Lv FQ4, Wang S5, Wang YR4, Luo YK4, Mei XG5, Tang J6. J Huazhong Univ Sci Technolog Med Sci. 2015 Oct;35(5):707-11. doi: 10.1007/s11596-015-1494-2. Epub 2015 Oct 22.
Gabexate mesilate (GM) is a trypsin inhibitor, and mainly used for treatment of various acute pancreatitis, including traumatic pancreatitis (TP), edematous pancreatitis, and acute necrotizing pancreatitis. However, due to the characteristics of pharmacokinetics, the clinical application of GM still needs frequently intravenous administration to keep the blood drug concentration, which is difficult to manage. Specially, when the blood supply of pancreas is directly damaged, intravenous administration is difficult to exert the optimum therapy effect. To address it, a novel thermosensitive in-situ gel of gabexate mesilate (GMTI) was developed, and the optimum formulation of GMTI containing 20.6% (w/w) P-407 and 5.79% (w/w) P188 with different concentrations of GM was used as a gelling solvent. The effective drug concentration on trypsin inhibition was examined after treatment with different concentrations of GMTI in vitro, and GM served as a positive control.
2.Effect of Somatostatin, Ulinastatin and Gabexate on the Treatment of Severe Acute Pancreatitis.
Wang G1, Liu Y2, Zhou SF3, Qiu P4, Xu L4, Wen P4, Wen J4, Xiao X5. Am J Med Sci. 2016 May;351(5):506-12. doi: 10.1016/j.amjms.2016.03.013. Epub 2016 Mar 31.
OBJECTIVE: The objective of this study is to evaluate the efficacy of somatostatin, ulinastatin and gabexate for the treatment of severe acute pancreatitis.
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CAS 56974-61-9 Gabexate mesylate

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