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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.

Items 26-29 of 29

  • XR 5118 hydrochloride
    Cat. No.
    A77012
    CAS No.
    174766-49-5

    XR 5118 hydrochloride

    XR 5118 hydrochloride is a selective inhibitor of plasminogen activator inhibitor 1 (PAI-1), with an IC50 value of 12 µM. By binding to PAI-1, XR 5118 hydrochloride effectively reduces plasma PAI-1 activity, promoting endogenous thrombolysis and inhibiting thrombus formation. This compound is valuable for research applications related to cancer and thrombotic disorders, providing insights into mechanisms of fibrinolysis and clot regulation.

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  • 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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  • WB 3559 A
    Cat. No.
    A77015
    CAS No.
    96053-97-3

    WB 3559 A

    WB 3559 A is a fibrinolytic plasminogen activator that enhances the conversion of plasminogen to plasmin, thereby facilitating the direct degradation of fibrin in thrombus formations. This compound exhibits significant potential in the study of acute thrombotic diseases, such as myocardial infarction and pulmonary embolism, making it a valuable tool for researchers investigating therapeutic strategies in vascular events and clot management.

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    25 mg
    $1,275.00
    All 1 sizes
  • D-Val-Leu-Arg-pNA hydrochloride
    Cat. No.
    A77016
    CAS No.
    1262750-87-7

    D-Val-Leu-Arg-pNA hydrochloride

    D-Val-Leu-Arg-pNA hydrochloride is a specific substrate for plasminogen activator inhibitor-1 (PAI-1). It is utilized to assess the enzymatic activities of plasminogen activators and plasmin. Additionally, this compound is valuable for investigating the fibrinolytic activity in various biological systems, including bacteria and nematodes, facilitating research in thrombosis and clot regulation.

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Items 26-29 of 29

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