SCH 79797 dihydrochloride

Cat. No. 1592

SCH 79797 dihydrochloride C23H25N5.2HCl [1216720-69-2]

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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.

Certificate of Analysis / Safety Data Sheet

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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.

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.

Ahn et al (1999) Structure-activity relationships of pyrroloquinazolines as thrombin receptor antagonists. Bioorg.Med.Chem.Lett. 9 2073. PMID: 10450984.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for SCH 79797 dihydrochloride include:

Tripathi et al (2014) Protease-activated receptor 2 (PAR2) is upregulated by Acanthamoeba plasminogen activator (aPA) and induces proinflammatory cytokine in human corneal epithelial cells. Invest Ophthalmol Vis Sci 55 3912. PMID: 24876278.

Yang et al (2014) Induction of tumor necrosis factor (TNF) release from subtypes of T cells by agonists of proteinase activated receptors. Mediators Inflamm 2013 165453. PMID: 24453410.

Juncker-Jensen et al (2013) Tumor MMP-1 activates endothelial PAR1 to facilitate vascular intravasation and metastatic dissemination. Cancer Res 73 4196. PMID: 23687338.

Chen et al (2012) Thrombin activity associated with neuronal damage during acute focal ischemia. J Neurosci 32 7622. PMID: 22649241.

Okamura et al (2011) A few immobilized thrombins are sufficient for platelet spreading. Biophys J 100 1855. PMID: 21504721.

Fujimoto et al (2010) The activation of Proteinase-Activated Receptor-1 (PAR1) mediates gastric cancer cell proliferation and invasion. BMC Cancer 10 443. PMID: 20723226.

Lee et al (2010) Alpha-synuclein activates microglia by inducing the expressions of matrix metalloproteinases and the subsequent activation of protease-activated receptor-1. J Immunol 185 615. PMID: 20511551.

Malik et al (2010) Plasma fibronectin promotes lung metastasis by contributions to fibrin clots and tumor cell invasion. Cancer Res 70 4327. PMID: 20501851.

Vidwan et al (2010) Activation of protease-activated receptors 3 and 4 accelerates tissue factor-induced thrombin generation on the surface of vascular smooth muscle cells. Arterioscler Thromb Vasc Biol 30 2587. PMID: 20930172.

Blackburn et al (2009) A matrix metalloproteinase-1/protease activated receptor-1 signaling axis promotes melanoma invasion and metastasis. Oncogene 28 4237. PMID: 19734937.

Popovic et al (2008) Thrombin-induced expression of endothelial CX3CL1 potentiates monocyte CCL2 production and transendothelial migration. J Leukoc Biol 84 215. PMID: 18436581.

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Keywords: SCH 79797 dihydrochloride, supplier, Potent, selective, non-peptide, PAR1, antagonists, PAR, Receptors, Protease-Activated, proteinase-activated, SCH79797, dihydrochloride, Tocris Bioscience, Protease-Activated Receptor Antagonist products

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