RWJ 56110

Cat. No. 2614

RWJ 56110 C41H43Cl2F2N7O3.2HCl [252889-88-6]

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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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Zania et al (2006) Blockade of angiogenesis by small molecule antagonists to protease-activated receptor-1: association with endothelial cell growth suppression and induction of apoptosis. J.Pharmacol.Exp.Ther. 318 246. PMID: 16595737.

Maryanoff et al (2003) Discovery of potent peptide-mimetic antagonists for the human thrombin receptor, protease-activated receptor-1 (PAR-1). Curr.Med.Chem.Cardiovasc.Hematol.Agents 1 13. PMID: 15317288.

Andrade-Gordon et al (1999) Design, synthesis and biological characterization of a peptide-mimetic antagonist for a tethered-ligand receptor. Proc.Natl.Acad.Sci.USA 96 12257. PMID: 10535908.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for RWJ 56110 include:

Xu et al (2015) Heat stress-induced disruption of endothelial barrier function is via PAR1 signaling and suppressed by Xuebijing injection. PLoS One 10 e0118057. PMID: 25693178.

Juncker-Jensen et al (2013) Tumor MMP-1 activates endothelial PAR1 to facilitate vascular intravasation and metastatic dissemination. Cancer Res 73 4196. PMID: 23687338.

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Keywords: RWJ 56110, supplier, selective, PAR1, antagonists, PAR, receptors, protease-activated, proteinase-activated, RWJ56110, Tocris Bioscience, Protease-Activated Receptor Antagonist products

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