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RWJ 56110

Cat. No. 2614

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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.

Resources

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch

Safety Data Sheet: View Safety Data Sheet

References

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.

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.

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.

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