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

Soluble to 25 mM in ethanol and to 50 mM in DMSO
>99 %
Desiccate at RT

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 / Product Datasheet / Safety Datasheet

Certificate of Analysis / Product Datasheet
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References are publications that support the products' biological activity.

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 SCH 79797 dihydrochloride please let us know.

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

Li et al (2016) Interference with protease-activated receptor 1 alleviates neuronal cell death induced by lipopolysaccharide-stimulated microglial cells through the PI3K/Akt pathway Nature Communications 6 38247. PMID: 27910893.

Carrim et al (2015) Thrombin-induced reactive oxygen species generation in platelets: A novel role for protease-activated receptor 4 and GPIbα. Proc Natl Acad Sci U S A 6 640. PMID: 26569550.

Gur-Cohen et al (2015) PAR1 signaling regulates the retention and recruitment of EPCR-expressing bone marrow hematopoietic stem cells. Int J Oncol 21 1307. PMID: 26457757.

Otsuki et al (2014) Thrombin conducts epithelial-mesenchymal transition via protease-activated receptor-1 in human gastric cancer. J Biol Chem 45 2287. PMID: 25231630.

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.

Gadepalli et al (2013) Novel role for p21-activated kinase 2 in thrombin-induced monocyte migration. Redox Biol 288 30815. PMID: 24025335.

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

Yan et al (2013) Role of SCH79797 in maintaining vascular integrity in rat model of subarachnoid hemorrhage. Nat Med 44 1410. PMID: 23539525.

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

Scarisbrick et al (2012) Kallikrein 6 is a novel molecular trigger of reactive astrogliosis. Cytotechnology 393 355. PMID: 22505518.

Dowal et al (2011) Identification of an antithrombotic allosteric modulator that acts through helix 8 of PAR1. J Neurosci 108 2951. PMID: 21282664.

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.

Yoshikawa et al (2010) Granzyme A and thrombin differentially promote the release of interleukin-8 from alveolar epithelial A549 cells. Proc Natl Acad Sci U S A 62 325. PMID: 20424914.

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.

Ma et al (2005) Proteinase-activated receptors 1 and 4 counter-regulate endostatin and VEGF release from human platelets. Biol Chem 102 216. PMID: 15615851.

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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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