RWJ 56110
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
Purity: ≥96%
Biological Activity
RWJ 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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Proteasome proteolysis supports stimulated platelet function and thrombosis.
Gupta N, Li W, Willard B, Silverstein R, McIntyre T
Arterioscler Thromb Vasc Biol, 2014;34(1):160-8. -
Tissue-type plasminogen activator neutralizes LPS but not protease-activated receptor-mediated inflammatory responses to plasmin
C Zalfa, P Azmoon, E Mantuano, SL Gonias
J. Leukoc. Biol., 2019;0(0):. -
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 -
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 -
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
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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
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Identification and therapeutic rescue of autophagosome and glutamate receptor defects in C9ORF72 and sporadic ALS neurons.
Authors: Shi Et al.
JCI Insight 2019;5
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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
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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
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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
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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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