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    Gabexate Mesylate (Megacert; Arodate)
    Gabexate Mesylate (Megacert; Arodate)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0709
    CAS #: 56974-61-9Purity ≥98%

    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.

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    Molecular Weight (MW)417.48
    FormulaC16H23N3O4.CH4O3S
    CAS No.56974-61-9
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 83 mg/mL (198.8 mM)
    Water: 12 mg/mL (28.7 mM)
    Ethanol: 83 mg/mL (198.8 mM)
    Other info

    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

    Synonyms

    Megacert; Mesyl Gabexate; gabexate mesilate; Arodate; Megacart; Gabexate; Gabexate mesylate; Arodate.


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    In Vitro

    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

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    References

    Biochem Biophys Res Commun. 1998 May 19;246(2):453-6.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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