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SCH 79797 dihydrochloride

Catalog #: 1592
28 Citations 1 Review Datasheet / COA / SDS
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1592/10
1592/50
SCH 79797 dihydrochloride | CAS No. 1216720-69-2 | Protease-Activated Receptor Antagonists
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Description: Potent, selective non-peptide PAR1 antagonist

Chemical Name: N3-Cyclopropyl-7-[[4-(1-methylethyl)phenyl]methyl]-7H-pyrrolo[3,2-f]quinazoline-1,3-diamine dihydrochloride

Purity: ≥99%

Product Details
Citations (28)
Supplemental Products
Reviews (1)
Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

SCH 79797 dihydrochloride is a potent, selective non-peptide PAR1 receptor antagonist (IC50 = 70 nM). Inhibits haTRAP-induced- but not γ-thrombin-, ADP- or collagen-induced human platelet aggregation. Selectively blocks PAR1 agonist- or thrombin-induced increases in cytosolic Ca2+ in vascular smooth muscle cells. Also broad spectrum antibiotic. Kills bacteria by a dual action of inhibiting dihydrofolate reductase and interfering with bacterial cell membrane integrity.

Technical Data

M.Wt:
444.41
Formula:
C23H25N5.2HCl
Solubility:
Soluble to 5 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. Granzyme B-induced neurotoxicity is mediated via activation of PAR-1 receptor and Kv1.3 channel.
    Wang, Tongguan, Lee, Myoung-H, Choi, Elliot, Pardo-Villamizar, Carlos A, Lee, Sung Bin, Yang, In Hong, Calabresi, Peter A, Nath, Avindra
    PLoS ONE, 2012;7(8):e43950.
  2. Factor VIIa binding to endothelial cell protein C receptor protects vascular barrier integrity in vivo.
    Sundaram, J, Keshava, S, Gopalakrishnan, R, Esmon, C T, Pendurthi, U R, Rao, L V M
    J Thromb Haemost, 2014;12(5):690-700.
  3. A novel function of FoxO transcription factors in thrombin-stimulated vascular smooth muscle cell proliferation.

    Thromb Haemost, 2012;108(1):148-58.
  4. Effect of thrombin on human amnion mesenchymal cells, mouse fetal membranes, and preterm birth.
    Mogami, Haruta, Keller, Patrick, Shi, Haolin, Word, R Ann
    J Biol Chem, 2014;289(19):13295-307.
  5. Protease signaling through protease activated receptor 1 mediate nerve activation by mucosal supernatants from irritable bowel syndrome but not from ulcerative colitis patients
    S Buhner, H Hahne, K Hartwig, Q Li, S Vignali, D Ostertag, C Meng, G Hörmannspe, B Braak, C Pehl, T Frieling, G Barbara, R De Giorgio, IE Demir, GO Ceyhan, F Zeller, G Boeckxstae, D Haller, B Kuster, M Schemann
    PLoS ONE, 2018;13(3):e0193943.
  6. Host gene-encoded severe lung TB: from genes to the potential pathways.
    Ganachari, M, Guio, H, Zhao, N, Flores-Villanueva, P O
    Genes Immun, 2012;13(8):605-20.
  7. A protease-activated receptor 1 antagonist protects against global cerebral ischemia/reperfusion injury after asphyxial cardiac arrest in rabbits
    JN Yang, J Chen, M Xiao
    Neural Regen Res, 2017;12(2):242-249.
  8. Structure-activity relationships of pyrroloquinazolines as thrombin receptor antagonists.
    Ahn et al.
    Bioorg.Med.Chem.Lett., 1999;9:2073
  9. 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
  10. 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
  11. A dual-mechanism antibiotic kills Gram-negative bacteria and avoids drug resistance.
    Martin et al.
    Cell, 2020;S0092-8674:30567

Product Datasheets

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Citations for SCH 79797 dihydrochloride

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

28 Citations: Showing 1 - 10

  1. Thrombin induces morphological and inflammatory astrocytic responses via activation of PAR1 receptor.
    Authors: Chen Et al.
    Cell Death Discov.  2022;8:189
  2. A dual-mechanism antibiotic kills Gram-negative bacteria and avoids drug resistance.
    Authors: Martin Et al.
    Cell  2020;S0092-8674:30567
  3. Cub domain-containing protein 1 negatively regulates TGF-β signaling and myofibroblast differentiation.
    Authors: Noskovičová Et al.
    Am J Physiol Lung Cell Mol Physiol  2018;314:L695
  4. PAR1?mediated c?Jun activation promotes heat stress?induced early stage apoptosis of human umbilical vein endothelial cells.
    Authors: Zhang Et al.
    Mol Med Rep  2017;15:2595
  5. 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
  6. PAR1 inhibition suppresses the self-renewal and growth of A2B5-defined glioma progenitor cells and their derived gliomas in vivo.
    Authors: Auvergne Et al.
    Oncogene  2016;35:3817
  7. Multiple Growth Factors, But Not VEGF, Stimulate Glycosaminoglycan Hyperelongation in Retinal Choroidal Endothelial Cells.
    Authors: Gwairi Et al.
    Int J Biol Sci  2016;12:1041
  8. 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
  9. 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
  10. 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
  11. Thrombin conducts epithelial-mesenchymal transition via protease-activated receptor-1 in human gastric cancer.
    Authors: Otsuki Et al.
    J Biol Chem  2014;45:2287
  12. 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
  13. Tumor MMP-1 activates endothelial PAR1 to facilitate vascular intravasation and metastatic dissemination.
    Authors: Juncker-Jensen Et al.
    Cancer Res  2013;73:4196
  14. Role of SCH79797 in maintaining vascular integrity in rat model of subarachnoid hemorrhage.
    Authors: Yan Et al.
    Nat Med  2013;44:1410
  15. Novel role for p21-activated kinase 2 in thrombin-induced monocyte migration.
    Authors: Gadepalli Et al.
    Redox Biol  2013;288:30815
  16. Kallikrein 6 is a novel molecular trigger of reactive astrogliosis.
    Authors: Scarisbrick Et al.
    Cytotechnology  2012;393:355
  17. Thrombin activity associated with neuronal damage during acute focal ischemia.
    Authors: Chen Et al.
    J Neurosci  2012;32:7622
  18. Host gene-encoded severe lung TB: from genes to the potential pathways.
    Authors: Ganachari Et al.
    Genes Immun  2012;13:605
  19. Identification of an antithrombotic allosteric modulator that acts through helix 8 of PAR1.
    Authors: Dowal Et al.
    J Neurosci  2011;108:2951
  20. A few immobilized thrombins are sufficient for platelet spreading.
    Authors: Okamura Et al.
    Biophys J  2011;100:1855
  21. Plasma fibronectin promotes lung metastasis by contributions to fibrin clots and tumor cell invasion.
    Authors: Malik Et al.
    Cancer Res  2010;70:4327
  22. 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
  23. 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
  24. 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
  25. The activation of Proteinase-Activated Receptor-1 (PAR1) mediates gastric cancer cell proliferation and invasion.
    Authors: Fujimoto Et al.
    BMC Cancer  2010;10:443
  26. A matrix metalloproteinase-1/protease activated receptor-1 signaling axis promotes melanoma invasion and metastasis.
    Authors: Blackburn Et al.
    Oncogene  2009;28:4237
  27. Thrombin-induced expression of endothelial CX3CL1 potentiates monocyte CCL2 production and transendothelial migration.
    Authors: Popovic Et al.
    J Leukoc Biol  2008;84:215
  28. Proteinase-activated receptors 1 and 4 counter-regulate endostatin and VEGF release from human platelets.
    Authors: Ma Et al.
    Biol Chem  2005;102:216

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Excellent inhibitor
By Anonymous on 03/18/2021
Species: Human

The experiment was aimed to test the thrombin activity in the blood plasma of KO mice. SCH 79797 was used at a concentration of 0.1 micro Molar.

Excellent inhibitor 1592
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