Catalog Number: 1592
Chemical Name: N3-Cyclopropyl-7-[[4-(1-methylethyl)phenyl]methyl]-7H-pyrrolo[3,2-f]quinazoline-1,3-diamine dihydrochloride
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
  • Solubility:
    Soluble to 25 mM in ethanol and to 50 mM in DMSO
  • Purity:
    >99%
  • Storage:
    Desiccate at RT
  • CAS No:
    1216720-69-2
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.
Background References
  1. Structure-activity relationships of pyrroloquinazolines as thrombin receptor antagonists.
    Ahn et al.
    Bioorg.Med.Chem.Lett., 1999;9:2073
  2. 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.
    Ahn et al.
    Biochem.Pharmacol., 2000;60:1425
  3. A role for proteinase-activated receptor 2 and PKC-ε in thrombin-mediated induction of decay-accelerating factor on human endothelial cells.
    Lidington et al.
    Am.J.Physiol.Cell Physiol., 2005;289:C1437
Citations:

The citations listed below are publications that use Tocris products. Selected citations for SCH 79797 dihydrochloride include:

21 Citations: Showing 1 - 10
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  1. Interference with protease-activated receptor 1 alleviates neuronal cell death induced by lipopolysaccharide-stimulated microglial cells through the PI3K/Akt pathway
    Authors: Li Et al.
    Nature Communications 2016;6:38247
  2. Thrombin-induced reactive oxygen species generation in platelets: A novel role for protease-activated receptor 4 and GPIbα.
    Authors: Carrim Et al.
    Proc Natl Acad Sci U S A 2015;6:640
  3. PAR1 signaling regulates the retention and recruitment of EPCR-expressing bone marrow hematopoietic stem cells.
    Authors: Gur-Cohen Et al.
    Int J Oncol 2015;21:1307
  4. Protease-activated receptor 2 (PAR2) is upregulated by Acanthamoeba plasminogen activator (aPA) and induces proinflammatory cytokine in human corneal epithelial cells.
    Authors: Tripathi Et al.
    Invest Ophthalmol Vis Sci 2014;55:3912
  5. Thrombin conducts epithelial-mesenchymal transition via protease-activated receptor-1 in human gastric cancer.
    Authors: Otsuki Et al.
    J Biol Chem 2014;45:2287
  6. Induction of tumor necrosis factor (TNF) release from subtypes of T cells by agonists of proteinase activated receptors.
    Authors: Yang Et al.
    Mediators Inflamm 2014;2013:165453
  7. Tumor MMP-1 activates endothelial PAR1 to facilitate vascular intravasation and metastatic dissemination.
    Authors: Juncker-Jensen Et al.
    Cancer Res 2013;73:4196
  8. Role of SCH79797 in maintaining vascular integrity in rat model of subarachnoid hemorrhage.
    Authors: Yan Et al.
    Nat Med 2013;44:1410
  9. Novel role for p21-activated kinase 2 in thrombin-induced monocyte migration.
    Authors: Gadepalli Et al.
    Redox Biol 2013;288:30815
  10. Kallikrein 6 is a novel molecular trigger of reactive astrogliosis.
    Authors: Scarisbrick Et al.
    Cytotechnology 2012;393:355
  11. Thrombin activity associated with neuronal damage during acute focal ischemia.
    Authors: Chen Et al.
    J Neurosci 2012;32:7622
  12. Identification of an antithrombotic allosteric modulator that acts through helix 8 of PAR1.
    Authors: Dowal Et al.
    J Neurosci 2011;108:2951
  13. A few immobilized thrombins are sufficient for platelet spreading.
    Authors: Okamura Et al.
    Biophys J 2011;100:1855
  14. Plasma fibronectin promotes lung metastasis by contributions to fibrin clots and tumor cell invasion.
    Authors: Malik Et al.
    Cancer Res 2010;70:4327
  15. Granzyme A and thrombin differentially promote the release of interleukin-8 from alveolar epithelial A549 cells.
    Authors: Yoshikawa Et al.
    Proc Natl Acad Sci U S A 2010;62:325
  16. Activation of protease-activated receptors 3 and 4 accelerates tissue factor-induced thrombin generation on the surface of vascular smooth muscle cells.
    Authors: Vidwan Et al.
    Arterioscler Thromb Vasc Biol 2010;30:2587
  17. Alpha-synuclein activates microglia by inducing the expressions of matrix metalloproteinases and the subsequent activation of protease-activated receptor-1.
    Authors: Lee Et al.
    J Immunol 2010;185:615
  18. The activation of Proteinase-Activated Receptor-1 (PAR1) mediates gastric cancer cell proliferation and invasion.
    Authors: Fujimoto Et al.
    BMC Cancer 2010;10:443
  19. A matrix metalloproteinase-1/protease activated receptor-1 signaling axis promotes melanoma invasion and metastasis.
    Authors: Blackburn Et al.
    Oncogene 2009;28:4237
  20. Thrombin-induced expression of endothelial CX3CL1 potentiates monocyte CCL2 production and transendothelial migration.
    Authors: Popovic Et al.
    J Leukoc Biol 2008;84:215
  21. Proteinase-activated receptors 1 and 4 counter-regulate endostatin and VEGF release from human platelets.
    Authors: Ma Et al.
    Biol Chem 2005;102:216
Expand to show all 21 Citations

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