Biological Activity
Potent, selective non-peptide PAR1 receptor antagonist (IC50 = 70 nM). Inhibits haTRAP-induced- but not γ-thrombin-, ADP- or collagen-induced human platelet aggregation. Also selectively blocks PAR1 agonist- or thrombin-induced increases in cytosolic Ca2+ in vascular smooth muscle cells.
Technical Data
| M. Wt | 444.41 |
| Formula | C23H25N5.2HCl |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 1216720-69-2 |
| PubChem ID | 45073452 |
| InChI Key | NNJTXSQXGHYXAJ-UHFFFAOYSA-N |
| Smiles | Cl.Cl.CC(C)C1=CC=C(CN2C=CC3=C2C=CC2=NC(NC4CC4)=NC(N)=C32)C=C1 |
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 | 22.22 | 50 | |
| ethanol | 11.11 | 25 |
Preparing Stock Solutions
The following data is based on the product molecular weight 444.41. 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 | 2.25 mL | 11.25 mL | 22.5 mL |
| 5 mM | 0.45 mL | 2.25 mL | 4.5 mL |
| 10 mM | 0.23 mL | 1.13 mL | 2.25 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.45 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Ahn et al (1999) Structure-activity relationships of pyrroloquinazolines as thrombin receptor antagonists. Bioorg.Med.Chem.Lett. 9 2073 PMID: 10450984
Ahn et al (2000) Inhibition of cellular action of thrombin by N3-cyclopropyl-7-{[4-(1-methylethyl)phenyl]methyl}-7H-pyrrolo[3,2-f]quinazoline-1,3-diamine (SCH 79797), a nonpeptide thrombin receptor antagonist. Biochem.Pharmacol. 60 1425 PMID: 11020444
Lidington et al (2005) A role for proteinase-activated receptor 2 and PKC-ε in thrombin-mediated induction of decay-accelerating factor on human endothelial cells. Am.J.Physiol.Cell Physiol. 289 C1437 PMID: 16079188
Keywords: SCH 79797 dihydrochloride, supplier, Potent, selective, non-peptide, PAR1, antagonists, PAR, Receptors, Protease-Activated, proteinase-activated, SCH79797, dihydrochloride, Protease-Activated, Receptors, Protease-Activated, Receptors, Tocris Bioscience
