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:
  • Formula:
  • Solubility:
    Soluble to 25 mM in ethanol and to 50 mM in DMSO
  • Purity:
  • Storage:
    Desiccate at RT
  • CAS No:
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

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

Showing Results 1 - 10 of 20

  1. 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
  2. PAR1 signaling regulates the retention and recruitment of EPCR-expressing bone marrow hematopoietic stem cells.
    Authors: Gur-Cohen Et al.
    Int J Oncol
  3. 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
  4. Thrombin conducts epithelial-mesenchymal transition via protease-activated receptor-1 in human gastric cancer.
    Authors: Otsuki Et al.
    J Biol Chem
  5. Induction of tumor necrosis factor (TNF) release from subtypes of T cells by agonists of proteinase activated receptors.
    Authors: Yang Et al.
    Mediators Inflamm
  6. Tumor MMP-1 activates endothelial PAR1 to facilitate vascular intravasation and metastatic dissemination.
    Authors: Juncker-Jensen Et al.
    Cancer Res
  7. Role of SCH79797 in maintaining vascular integrity in rat model of subarachnoid hemorrhage.
    Authors: Yan Et al.
    Nat Med
  8. Novel role for p21-activated kinase 2 in thrombin-induced monocyte migration.
    Authors: Gadepalli Et al.
    Redox Biol
  9. Kallikrein 6 is a novel molecular trigger of reactive astrogliosis.
    Authors: Scarisbrick Et al.
  10. Thrombin activity associated with neuronal damage during acute focal ischemia.
    Authors: Chen Et al.
    J Neurosci
  11. Identification of an antithrombotic allosteric modulator that acts through helix 8 of PAR1.
    Authors: Dowal Et al.
    J Neurosci
  12. A few immobilized thrombins are sufficient for platelet spreading.
    Authors: Okamura Et al.
    Biophys J
  13. Plasma fibronectin promotes lung metastasis by contributions to fibrin clots and tumor cell invasion.
    Authors: Malik Et al.
    Cancer Res
  14. 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
  15. 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
  16. 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
  17. The activation of Proteinase-Activated Receptor-1 (PAR1) mediates gastric cancer cell proliferation and invasion.
    Authors: Fujimoto Et al.
    BMC Cancer
  18. A matrix metalloproteinase-1/protease activated receptor-1 signaling axis promotes melanoma invasion and metastasis.
    Authors: Blackburn Et al.
  19. Thrombin-induced expression of endothelial CX3CL1 potentiates monocyte CCL2 production and transendothelial migration.
    Authors: Popovic Et al.
    J Leukoc Biol
  20. Proteinase-activated receptors 1 and 4 counter-regulate endostatin and VEGF release from human platelets.
    Authors: Ma Et al.
    Biol Chem
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