Catalog Number: 2614
Chemical Name: (αS)-N-[(1S)-3-Amino-1-[[(phenylmethyl)amino]carbonyl]propyl]-α-[[[[1-[(2,6-dichlorophenyl)methyl]-3-(1-pyrrolidinylmethyl)-1H-indol-6-yl]amino]carbonyl]amino]-3,4-difluoro-benzenepropanamide
Biological Activity
Selective protease-activated receptor-1 (PAR1) antagonist; displays no activity at PAR2, PAR3, or PAR4 subtypes. Blocks thrombin-induced platelet aggregation and activation of MAPK in HUVECs. Also inhibits angiogenesis in a chick embryo angiogenesis model in vivo.
Technical Data
  • M.Wt:
    863.65
  • Formula:
    C41H43Cl2F2N7O3.2HCl
  • Solubility:
    Soluble to 25 mM in water and to 100 mM in DMSO
  • Purity:
    >96%
  • Storage:
    Store at -20°C
  • CAS No:
    252889-88-6
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Design, synthesis and biological characterization of a peptide-mimetic antagonist for a tethered-ligand receptor.
    Andrade-Gordon et al.
    Proc.Natl.Acad.Sci.USA, 1999;96:12257
  2. Discovery of potent peptide-mimetic antagonists for the human thrombin receptor, protease-activated receptor-1 (PAR-1).
    Maryanoff et al.
    Curr.Med.Chem.Cardiovasc.Hematol.Agents, 2003;1:13
  3. Blockade of angiogenesis by small molecule antagonists to protease-activated receptor-1: association with endothelial cell growth suppression and induction of apoptosis.
    Zania et al.
    J.Pharmacol.Exp.Ther., 2006;318:246
Citations:

The citations listed below are publications that use Tocris products. Selected citations for RWJ 56110 include:

3 Citations: Showing 1 - 3
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  1. Complement-activation fragment C4a mediates effector functions by binding as untethered agonist to protease-activated receptors 1 and 4.
    Authors: Wang
    Proc Natl Acad Sci U S A 2017;114(41):10948
  2. Heat stress-induced disruption of endothelial barrier function is via PAR1 signaling and suppressed by Xuebijing injection.
    Authors: Xu Et al.
    PLoS One 2015;10:e0118057
  3. Tumor MMP-1 activates endothelial PAR1 to facilitate vascular intravasation and metastatic dissemination.
    Authors: Juncker-Jensen Et al.
    Cancer Res 2013;73:4196

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