Argatroban

- Overview
  - Argatroban is a synthetic small molecule and potent thrombin inhibitor that functions as an anticoagulant agent. It can protect against thrombosis by limiting clot formation.
    
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    Background
    
    Argatroban is able to inhibit thrombin directly and univalently. The Ki values against thrombin range from 5 nM to 39 nM.
- Properties
  - Categories
    
    BioActive Small Molecules
    
    CAS Number
    
    74863-84-6
    
    Molecular Formula
    
    C23H36N6O5S
    
    Molecular Weight
    
    508.63
    
    Appearance
    
    White to off-white crystalline powder
    
    Solubility
    
    Slightly soluble in methanol, ethanol, DMF and DMSO.
    
    Other Properties
    
    Source: Synthetic
    Purity Level: ≥98% (anhydrous basis)
    
    Storage
    
    -20°C
    
    * For research use only
- Applications
  - Application Description
    
    Eukaryotic Cell Culture Applications: Argatroban was applied to cultured rabbit aortic vascular smooth muscle cells, and the expression of myosin heavy-chain isoform mRNAs was evaluated. Authors found mRNA was homogenously expressed, thus inducing the phenotypic conversion of vascular smooth muscle cells (Yoshinaga et al, 2003). The effect of Argatroban on endothelial cells experimentall injured by thrombin were investigated using cell line TKM-33 cloned from human umbilical vein endothelial cells. Endothelial cells make plasminogen activator to maintain blood flow and prevent thrombosis. The treatment with Argatroban prior to thrombin injury resulted in the induction of plasminogen activator inhibitor-1 (PAI-1) secretion. Thus, Argatroban pretreatment can prevent thrombin injury of endothelial cells (Ueshima et al, 2000).
    
    Cancer Applications: Argatroban was found to reduce breast cancer malignancy and metastatis in MDA-MB-468 human breast cancer cells that were stably transfected to overexpress osteopontin. Argatroban treatment of 25 µg/ml resulted in decreased cell growth, colony-forming ability, adhesion, and migration (Schulze et al, 2008).