Name: AR-C 66096 tetrasodium salt
Price: 817.00 USD

- Overview
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    Background
    
    The platelet P2T receptor plays a major role in platelet aggregation, and its antagonists are suggested to have significant therapeutic potential as antithrombotic agents. AR-C 66096 is a novel, potent and selective antagonist at human platelet P2T-purinoceptors.In vitro: In suspensions of human washed platelets, AR-C 66096 (1-100 nM) produced concentrationdependent rightward displacement of concentration-effect (E/[A]) curves obtained for ADP-induced platelet aggregation. The anti-aggregatory potency of AR-C 66096 was not influenced by increasing the incubation time from 2 to 15 min nor by inclusion of the P1-purinoceptor antagonist 8-sulphophenyltheophylline at a concentration (300 μM) [1]. In vivo: AR-C 66096 behaved as a weak (pA50 3.68) but full P2x-purinoceptor agonist in preparations of the isolated rabbit ear artery and as a weak, competitive antagonist (apparent pKB 4.71) at P2Y-purinoceptors in the isolated guinea-pig aorta, indicating a selectivity of at least 9000 fold for the Pzrsubtype. In the latter preparation, non-specific relaxations were observed by concentrations of AR-C 66096 >10 μM [1]. Clinical trial: Up to now, AR-C 66096 is still in the preclinical development stage.
- Properties
  - Categories
    
    P2Y12 antagonist, potent and selective
    
    CAS Number
    
    145782-74-7
    
    Molecular Formula
    
    C14H18F2N5Na4O12P3S
    
    Molecular Weight
    
    703.26
    
    Appearance
    
    Colourless liquid
    
    Purity
    
    98.00%
    
    Solubility
    
    <10mM in H2O
    
    Storage
    
    Store at -20°C
    
    SMILES
    
    CCCSC1=NC(N)=C(N=CN2[[email protected]@]3([H])[[email protected]](O)([H])[[email protected]@](O)([H])[[email protected]@](O3)([H])COP([O-])(OP(C(F)(P([O-])([O-])=O)F)([O-])=O)=O)C2=N1.[Na+].[Na+].[Na+].[Na+]
    
    * For Research Use Only