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 ActivityRWJ 56110 is a 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Discovery of potent peptide-mimetic antagonists for the human thrombin receptor, protease-activated receptor-1 (PAR-1).
Maryanoff et al.
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.
Design, synthesis and biological characterization of a peptide-mimetic antagonist for a tethered-ligand receptor.
Andrade-Gordon et al.
Citations for RWJ 56110
The citations listed below are publications that use Tocris products. Selected citations for RWJ 56110 include:
5 Citations: Showing 1 - 5
Identification and therapeutic rescue of autophagosome and glutamate receptor defects in C9ORF72 and sporadic ALS neurons.
Authors: Shi Et al.
JCI Insight 2019;5
Complement-activation fragment C4a mediates effector functions by binding as untethered agonist to protease-activated receptors 1 and 4.
Proc Natl Acad Sci U S A 2017;114(41):10948
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
Disruption of epithelial barrier by quorum-sensing N-3-(oxododecanoyl)-homoserine lactone is mediated by matrix metalloproteinases.
Authors: Eum Et al.
Am J Physiol Gastrointest Liver Physiol 2014;306:G992
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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