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 |
| Storage | Store at -20°C |
| Purity | ≥96% (HPLC) |
| CAS Number | 252889-88-6 |
| 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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 86.36 | 100 | |
| water | 21.59 | 25 |
Preparing Stock Solutions
The following data is based on the product molecular weight 863.65. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.16 mL | 5.79 mL | 11.58 mL |
| 5 mM | 0.23 mL | 1.16 mL | 2.32 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.16 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
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
Keywords: RWJ 56110, supplier, selective, PAR1, antagonists, PAR, receptors, protease-activated, proteinase-activated, RWJ56110, Protease-Activated, Receptors, Protease-Activated, Receptors, Tocris Bioscience
