423735-93-7

Usage

Uses

Used in Pharmaceutical Industry:
ML 161 is used as a selective inhibitor for platelet activation at protease-activated receptor 1 (PAR1) for the prevention and treatment of conditions related to excessive platelet activation, such as thrombosis and other clot-related disorders.
Used in Research Applications:
ML 161 is used as a research tool to study the role of PAR1 in platelet activation and thrombin-induced responses. It helps researchers understand the underlying mechanisms of platelet activation and develop new therapeutic strategies for related conditions.

references

[1]. dockendorff, c., et al., discovery of 1,3-diaminobenzenes as selective inhibitors of platelet activation at the par1 receptor. acs med chem lett, 2012. 3(3): p. 232-237.[2]. verplank, l., et al., chemical genetic analysis of platelet granule secretion-probe 3, in probe reports from the nih molecular libraries program. 2010, national center for biotechnology information (us): bethesda (md).

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Relevant academic research and scientific papers

Compounds and methods for treating diseases mediated by protease activated receptors

The invention relates to the use of a compound of Formula I for the treatment of protease-activated receptor mediated diseases by the administration of a compound of Formula I or a prodrug or metabolite thereof.

Discovery of 1,3-diaminobenzenes as selective inhibitors of platelet activation at the PAR1 receptor

A high-throughput screen of the NIH-MLSMR compound collection, along with a series of secondary assays to identify potential targets of hit compounds, previously identified a 1,3-diaminobenzene scaffold that targets protease-activated receptor 1 (PAR1). We now report additional structure-activity relationship (SAR) studies that delineate the requirements for activity at PAR1 and identify plasma-stable analogues with nanomolar inhibition of PAR1-mediated platelet activation. Compound 4 was declared as a probe (ML161) with the NIH Molecular Libraries Program. This compound inhibited platelet aggregation induced by a PAR1 peptide agonist or by thrombin but not by several other platelet agonists. Initial studies suggest that ML161 is an allosteric inhibitor of PAR1. These findings may be important for the discovery of antithrombotics with an improved safety profile.