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Submit ReviewRWJ 56110
Description: Selective PAR1 antagonist
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% (HPLC)
Biological Activity for RWJ 56110
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 for RWJ 56110
| M. Wt | 863.65 |
| Formula | C41H43Cl2F2N7O3.2HCl |
| Storage | Store at -20°C |
| Purity | ≥96% (HPLC) |
| CAS Number | 2387505-58-8 |
| PubChem ID | 90488773 |
| InChI Key | MGZSVSHDIOPSBO-ZEUUMAKDSA-N |
| Smiles | ClC1=CC=CC(Cl)=C1CN3C2=CC(NC(N[C@@H](CC5=CC(F)=C(F)C=C5)C(N[C@@H](CCN)C(NCC6=CC=CC=C6)=O)=O)=O)=CC=C2C(CN4CCCC4)=C3.Cl.Cl |
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.
Product Datasheets for RWJ 56110
References for RWJ 56110
References are publications that support the biological activity of the product.
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
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
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Keywords: RWJ 56110, RWJ 56110 supplier, selective, PAR1, antagonists, PAR, receptors, protease-activated, proteinase-activated, RWJ56110, 252889-88-6, Protease-Activated, Receptors, 2614, Tocris Bioscience
5 Citations for RWJ 56110
Citations are publications that use Tocris products. Selected citations for RWJ 56110 include:
Shi et al (2019) Identification and therapeutic rescue of autophagosome and glutamate receptor defects in C9ORF72 and sporadic ALS neurons. JCI Insight 5 PMID: 31310593
Wang (2017) 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 114 10948 PMID: 28973891
Juncker-Jensen et al (2013) Tumor MMP-1 activates endothelial PAR1 to facilitate vascular intravasation and metastatic dissemination. Cancer Res 73 4196 PMID: 23687338
Eum et al (2014) Disruption of epithelial barrier by quorum-sensing N-3-(oxododecanoyl)-homoserine lactone is mediated by matrix metalloproteinases. Am J Physiol Gastrointest Liver Physiol 306 G992 PMID: 24742991
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
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