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PAI-1

PAI-1 inhibitors act on plasminogen activator inhibitor 1, the main brake on fibrinolysis. PAI-1, encoded by serpin family E member 1 (SERPINE1), is a serine protease inhibitor (serpin). It inactivates tissue-type and urokinase-type plasminogen activators (tPA, uPA), which convert plasminogen into the fibrin-degrading protease plasmin. Active PAI-1 converts spontaneously into an inactive latent form, so its activity in samples changes over time. Raised PAI-1 has been linked to thrombosis, obesity and tissue fibrosis, which are studied in animal models. Tiplaxtinin (PAI-039), TM5275 sodium and TM5441 are small-molecule PAI-1 inhibitors that restore plasminogen activator activity. UK-371804 and ZK824859 instead inhibit uPA, acting on the protease rather than its inhibitor.

2 Items

  • D-Val-Leu-Arg-pNA
    Cat. No.
    A77007
    CAS No.
    64816-14-4

    D-Val-Leu-Arg-pNA

    D-Val-Leu-Arg-pNA is a substrate for glandular kininoreleasing enzymes and tissue-type plasminogen activator (t-PA), exhibiting no significant affinity for fibrin. This compound is utilized to study enzyme kinetics and the activation mechanisms of proteolytic enzymes involved in various physiological processes. Its specificity for t-PA makes it a valuable tool in research focusing on thrombolytic therapy and related areas.

    In stock View Details
    1 mg
    $85.00
    5 mg
    $215.00
    All 3 sizes
  • D-Val-Leu-Lys-AMC
    Cat. No.
    A77014
    CAS No.
    148168-23-4

    D-Val-Leu-Lys-AMC

    D-Val-Leu-Lys-AMC is a selective fluorogenic peptide substrate for plasmin, enabling the quantification of its enzymatic activity. This compound exhibits increased fluorescence upon cleavage, facilitating studies in fibrinolysis and related processes. It is suitable for applications in enzyme activity assays, offering high sensitivity with excitation at 360-380 nm and emission at 440-460 nm.

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    Out of stock

    All 3 sizes

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