SCH 79797 dihydrochloride

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Cat.No. 1592 - SCH 79797 dihydrochloride | C23H25N5.2HCl | CAS No. 1216720-69-2
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% (HPLC)
Datasheet
Citations (21)
Literature

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
Storage Desiccate at RT
Purity ≥99% (HPLC)
CAS Number 1216720-69-2
PubChem ID 45073452
InChI Key NNJTXSQXGHYXAJ-UHFFFAOYSA-N
Smiles Cl.Cl.CC(C)C1=CC=C(CN2C=CC3=C2C=CC2=NC(NC4CC4)=NC(N)=C32)C=C1

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 22.22 50
ethanol 11.11 25

Preparing Stock Solutions

The following data is based on the product molecular weight 444.41. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.25 mL 11.25 mL 22.5 mL
5 mM 0.45 mL 2.25 mL 4.5 mL
10 mM 0.23 mL 1.13 mL 2.25 mL
50 mM 0.05 mL 0.23 mL 0.45 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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

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

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


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

21 Citations for SCH 79797 dihydrochloride

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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


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