217313-79-6

Usage

Uses

Used in Pharmaceutical Research:
4-AMINOMETHYL BENZAMIDINE DIHYDROCHLORIDE is used as a research tool for studying the mechanisms of serine proteases, specifically targeting thrombin, which plays a crucial role in the coagulation cascade.
Used in Thrombotic Disorder Treatment:
In the medical field, 4-AMINOMETHYL BENZAMIDINE DIHYDROCHLORIDE is used as a potential therapeutic agent for the treatment of thrombotic disorders, leveraging its inhibitory effects on key components of blood clotting.
Used in Cardiovascular Disease Management:
4-AMINOMETHYL BENZAMIDINE DIHYDROCHLORIDE is utilized as a potential treatment for cardiovascular diseases, where its ability to inhibit clot formation can help prevent complications associated with these conditions.
Used in Antithrombotic Drug Development:
4-AMINOMETHYL BENZAMIDINE DIHYDROCHLORIDE is used as a lead compound in the development of new antithrombotic drugs, given its demonstrated potential to reduce the risk of blood clot formation.
Used in Scientific Studies:
In the scientific community, 4-AMINOMETHYL BENZAMIDINE DIHYDROCHLORIDE is employed as a specific inhibitor in experiments aimed at understanding and manipulating the activity of serine proteases, contributing to broader insights into related biological processes and diseases.

InChI:InChI=1/C8H11N3/c9-5-6-1-3-7(4-2-6)8(10)11/h1-4H,5,9H2,(H3,10,11)/p+2

Upstream product

• 162696-15-3 N-Boc-4-aminomethyl benzamidine 

Downstream Products

• 1456610-65-3 C₃₁H₄₆N₁₂O₄ 
• 1456610-68-6 C₂₇H₄₀N₁₀O₄S 
• 701270-17-9 4-amidinobenzylamine dihydrochloride 

Relevant academic research and scientific papers

Design, Synthesis, and Testing of Potent, Selective Hepsin Inhibitors via Application of an Automated Closed-Loop Optimization Platform

Hepsin is a membrane-anchored serine protease whose role in hepatocyte growth factor (HGF) signaling and epithelial integrity makes it a target of therapeutic interest in carcinogenesis and metastasis. Using an integrated design, synthesis, and screening platform, we were able to rapidly develop potent and selective inhibitors of hepsin. In progressing from the initial hit 7 to compound 53, the IC50 value against hepsin was improved from ～1 μM to 22 nM, and the selectivity over urokinase-type plasminogen activator (uPA) was increased from 30-fold to >6000-fold. Subsequent in vitro ADMET profiling and cellular studies confirmed that the leading compounds are useful tools for interrogating the role of hepsin in breast tumorigenesis.

Identification of the first low-molecular-weight inhibitors of matriptase-2

As recently discovered, matriptase-2, a type II transmembrane serine protease, plays a crucial role in body iron homeostasis by down-regulating hepcidin expression, which results in increased iron levels. Thus, matriptase-2 represents a novel target for the development of enzyme inhibitors potentially useful for the treatment of systemic iron overload (hemochromatosis). A comparative three-dimensional model of the catalytic domain of matriptase-2 was generated and utilized for structure-based virtual screening in combination with similarity searching and knowledge-based compound design. Two N-protected dipeptide amides containing a 4-amidinobenzylamide as P1 residue (compounds 1 and 3) were identified as the first small molecule inhibitors of matriptase-2 with Ki values of 170 and 460 nM, respectively. An inhibitor of the closely related protease matriptase (compound 2, Ki = 220 nM), with more than 50-fold selectivity over matriptase-2, was also identified.

Novel compounds that inhibit tryptase activity

The present invention relates to compounds of the Formula or a pharmaceutically acceptable salt, solvate, hydrate or formulation thereof. These compounds can be used for the inhibition of tryptase and for the treatment and/or prevention of diseases that a