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company name :
Tocris Bioscience
product type :
chemical
product name :
SCH 79797 dihydrochloride
catalog :
1592/10
quantity :
10 mg (also 50 mg)
price :
333 USD
more info or order :
citations: 34
Reference
Chen X, Zhang H, Hao H, Zhang X, Song H, He B, et al. Thrombin induces morphological and inflammatory astrocytic responses via activation of PAR1 receptor. Cell Death Discov. 2022;8:189 pubmed publisher
Martin J, Sheehan J, Bratton B, Moore G, Mateus A, Li S, et al. A Dual-Mechanism Antibiotic Kills Gram-Negative Bacteria and Avoids Drug Resistance. Cell. 2020;181:1518-1532.e14 pubmed publisher
Buhner S, Hahne H, Hartwig K, Li Q, Vignali S, Ostertag D, et al. Protease signaling through protease activated receptor 1 mediate nerve activation by mucosal supernatants from irritable bowel syndrome but not from ulcerative colitis patients. PLoS ONE. 2018;13:e0193943 pubmed publisher
Noskovičová N, Heinzelmann K, Burgstaller G, Behr J, Eickelberg O. Cub domain-containing protein 1 negatively regulates TGF-β signaling and myofibroblast differentiation. Am J Physiol Lung Cell Mol Physiol. 2018;314:L695-L707 pubmed publisher
Zhang S, Liu Y, WANG Z, Liu J, Gu Z, Xu Q, et al. PAR1‑mediated c‑Jun activation promotes heat stress‑induced early stage apoptosis of human umbilical vein endothelial cells. Mol Med Rep. 2017;15:2595-2603 pubmed publisher
Yang J, Chen J, Xiao M. A protease-activated receptor 1 antagonist protects against global cerebral ischemia/reperfusion injury after asphyxial cardiac arrest in rabbits. Neural Regen Res. 2017;12:242-249 pubmed publisher
Li Y, Yang W, Quinones Hinojosa A, Wang B, Xu S, Zhu W, et al. Interference with Protease-activated Receptor 1 Alleviates Neuronal Cell Death Induced by Lipopolysaccharide-Stimulated Microglial Cells through the PI3K/Akt Pathway. Sci Rep. 2016;6:38247 pubmed publisher
Al Gwairi O, Osman N, Getachew R, Zheng W, Liang X, Kamato D, et al. Multiple Growth Factors, But Not VEGF, Stimulate Glycosaminoglycan Hyperelongation in Retinal Choroidal Endothelial Cells. Int J Biol Sci. 2016;12:1041-51 pubmed publisher
Auvergne R, Wu C, Connell A, Au S, Cornwell A, Osipovitch M, et al. PAR1 inhibition suppresses the self-renewal and growth of A2B5-defined glioma progenitor cells and their derived gliomas in vivo. Oncogene. 2016;35:3817-28 pubmed publisher
Carrim N, Arthur J, Hamilton J, Gardiner E, Andrews R, Moran N, et al. Thrombin-induced reactive oxygen species generation in platelets: A novel role for protease-activated receptor 4 and GPIbα. Redox Biol. 2015;6:640-647 pubmed publisher
Gur Cohen S, Itkin T, Chakrabarty S, Graf C, Kollet O, Ludin A, et al. PAR1 signaling regulates the retention and recruitment of EPCR-expressing bone marrow hematopoietic stem cells. Nat Med. 2015;21:1307-17 pubmed publisher
Otsuki T, Fujimoto D, Hirono Y, Goi T, Yamaguchi A. Thrombin conducts epithelial‑mesenchymal transition via protease‑activated receptor‑1 in human gastric cancer. Int J Oncol. 2014;45:2287-94 pubmed publisher
Sundaram J, Keshava S, Gopalakrishnan R, Esmon C, Pendurthi U, Rao L. Factor VIIa binding to endothelial cell protein C receptor protects vascular barrier integrity in vivo. J Thromb Haemost. 2014;12:690-700 pubmed
Tripathi T, Abdi M, Alizadeh H. 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. 2014;55:3912-21 pubmed publisher
Mogami H, Keller P, Shi H, Word R. Effect of thrombin on human amnion mesenchymal cells, mouse fetal membranes, and preterm birth. J Biol Chem. 2014;289:13295-307 pubmed publisher
Yang H, Li T, Wei J, Zhang H, He S. Induction of tumor necrosis factor (TNF) release from subtypes of T cells by agonists of proteinase activated receptors. Mediators Inflamm. 2013;2013:165453 pubmed publisher
Gadepalli R, Kotla S, Heckle M, Verma S, Singh N, Rao G. Novel role for p21-activated kinase 2 in thrombin-induced monocyte migration. J Biol Chem. 2013;288:30815-31 pubmed publisher
Juncker Jensen A, Deryugina E, Rimann I, Zajac E, Kupriyanova T, Engelholm L, et al. Tumor MMP-1 activates endothelial PAR1 to facilitate vascular intravasation and metastatic dissemination. Cancer Res. 2013;73:4196-211 pubmed publisher
Yan J, Manaenko A, Chen S, Klebe D, Ma Q, Caner B, et al. Role of SCH79797 in maintaining vascular integrity in rat model of subarachnoid hemorrhage. Stroke. 2013;44:1410-7 pubmed publisher
Ganachari M, Guio H, Zhao N, Flores Villanueva P. Host gene-encoded severe lung TB: from genes to the potential pathways. Genes Immun. 2012;13:605-20 pubmed publisher
Wang T, Lee M, Choi E, Pardo Villamizar C, Lee S, Yang I, et al. Granzyme B-induced neurotoxicity is mediated via activation of PAR-1 receptor and Kv1.3 channel. PLoS ONE. 2012;7:e43950 pubmed publisher
Chen B, Friedman B, Whitney M, Winkle J, Lei I, Olson E, et al. Thrombin activity associated with neuronal damage during acute focal ischemia. J Neurosci. 2012;32:7622-31 pubmed publisher
Mahajan S, Fender A, Meyer Kirchrath J, Kurt M, Barth M, Sagban T, et al. A novel function of FoxO transcription factors in thrombin-stimulated vascular smooth muscle cell proliferation. Thromb Haemost. 2012;108:148-58 pubmed publisher
Scarisbrick I, Radulovic M, Burda J, Larson N, Blaber S, Giannini C, et al. Kallikrein 6 is a novel molecular trigger of reactive astrogliosis. Biol Chem. 2012;393:355-67 pubmed publisher
Okamura Y, Schmidt R, Raschke I, Hintze M, Takeoka S, Egner A, et al. A few immobilized thrombins are sufficient for platelet spreading. Biophys J. 2011;100:1855-63 pubmed publisher
Dowal L, Sim D, Dilks J, Blair P, Beaudry S, Denker B, et al. Identification of an antithrombotic allosteric modulator that acts through helix 8 of PAR1. Proc Natl Acad Sci U S A. 2011;108:2951-6 pubmed publisher
Vidwan P, Pathak A, Sheth S, Huang J, Monroe D, Stouffer G. 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. 2010;30:2587-96 pubmed publisher
Fujimoto D, Hirono Y, Goi T, Katayama K, Matsukawa S, Yamaguchi A. The activation of Proteinase-Activated Receptor-1 (PAR1) mediates gastric cancer cell proliferation and invasion. BMC Cancer. 2010;10:443 pubmed publisher
Lee E, Woo M, Moon P, Baek M, Choi I, Kim W, et al. Alpha-synuclein activates microglia by inducing the expressions of matrix metalloproteinases and the subsequent activation of protease-activated receptor-1. J Immunol. 2010;185:615-23 pubmed publisher
Malik G, Knowles L, Dhir R, Xu S, Yang S, Ruoslahti E, et al. Plasma fibronectin promotes lung metastasis by contributions to fibrin clots and tumor cell invasion. Cancer Res. 2010;70:4327-34 pubmed publisher
Yoshikawa Y, Hirayasu H, Tsuzuki S, Fushiki T. Granzyme A and thrombin differentially promote the release of interleukin-8 from alveolar epithelial A549 cells. Cytotechnology. 2010;62:325-32 pubmed publisher
Blackburn J, Liu I, Coon C, Brinckerhoff C. A matrix metalloproteinase-1/protease activated receptor-1 signaling axis promotes melanoma invasion and metastasis. Oncogene. 2009;28:4237-48 pubmed publisher
Popovic M, Laumonnier Y, Burysek L, Syrovets T, Simmet T. Thrombin-induced expression of endothelial CX3CL1 potentiates monocyte CCL2 production and transendothelial migration. J Leukoc Biol. 2008;84:215-23 pubmed publisher
Ma L, Perini R, McKnight W, Dicay M, Klein A, Hollenberg M, et al. Proteinase-activated receptors 1 and 4 counter-regulate endostatin and VEGF release from human platelets. Proc Natl Acad Sci U S A. 2005;102:216-20 pubmed
product information
brand :
Tocris, a Bio-Techne brand
catalog number base :
1592
SKU :
1592/10
product name :
SCH 79797 dihydrochloride
description :
Potent, selective non-peptide PAR1 antagonist
target :
Protease-Activated Receptor Antagonists
unit size :
10 mg (also 50 mg)
category :
Small Molecules
purity :
99%
storage :
Desiccate at RT
observed molecular weight :
444.41
url print :
?utm_source=biocompare&utm_medium=referral&utm_campaign=product&utm_term=smallmolecules
details of functionality :
SCH 79797 dihydrochloride is a potent, selective non-peptide PAR1 receptor antagonist (IC50 = 70 nM). Inhibits haTRAP-induced- but not -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.
product keywords :
Potent selective non-peptide PAR1 antagonists PAR Receptors Protease-Activated proteinase-activated SCH79797 dihydrochloride dihydrofolate reductase DHFR inhibitors inhibits broad spectrum antibiotic bacterial membrane integrity Protease-Activated Receptors Antibiotics Dihydrofolate Reductase 1592,
extended description :
Potent, selective non-peptide PAR1 antagonist
chemical name text :
N3-Cyclopropyl-7-[[4-(1-methylethyl)phenyl]methyl]-7H-pyrrolo[3,2-f]quinazoline-1,3-diamine dihydrochloride
formula :
C23H25N5.2HCl
formula text :
C23H25N5.2HCl
cas num :
1216720-69-2
USD :
319
USD 2025 :
333 USD
product details :
Potent, selective non-peptide PAR1 antagonist
more info or order :
company information
Tocris Bioscience
The Watkins Building
Atlantic Road
Avonmouth, Bristol
BS11 9QD
info@bio-techne.com
https://www.tocris.com
800-343-7475
headquarters: UK