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Submit ReviewSCH 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.
SCH 79797 dihydrochloride is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 444.41 |
公式 | C23H25N5.2HCl |
储存 | Desiccate at RT |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
ethanol | 2.22 | 5 | |
DMSO | 22.22 | 50 |
以下数据基于产品分子量 444.41。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.5 mM | 4.5 mL | 22.5 mL | 45 mL |
2.5 mM | 0.9 mL | 4.5 mL | 9 mL |
5 mM | 0.45 mL | 2.25 mL | 4.5 mL |
25 mM | 0.09 mL | 0.45 mL | 0.9 mL |
参考文献是支持产品生物活性的出版物。
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
Martin et al (2020) A dual-mechanism antibiotic kills Gram-negative bacteria and avoids drug resistance. Cell S0092-8674 30567 PMID: 32497502
If you know of a relevant reference for SCH 79797 dihydrochloride, please let us know.
关键词: SCH 79797 dihydrochloride, SCH 79797 dihydrochloride supplier, 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, Antibiotics, Dihydrofolate, Reductase, 1592, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 SCH 79797 dihydrochloride 的部分引用包括:
Martin et al (2020) A dual-mechanism antibiotic kills Gram-negative bacteria and avoids drug resistance. Cell S0092-8674 30567 PMID: 32497502
Okamura et al (2011) A few immobilized thrombins are sufficient for platelet spreading. Biophys J 100 1855 PMID: 21504721
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
Ganachari et al (2012) Host gene-encoded severe lung TB: from genes to the potential pathways. Genes Immun 13 605 PMID: 22992722
Blackburn et al (2009) A matrix metalloproteinase-1/protease activated receptor-1 signaling axis promotes melanoma invasion and metastasis. Oncogene 28 4237 PMID: 19734937
Zhang et al (2017) PAR1?mediated c?Jun activation promotes heat stress?induced early stage apoptosis of human umbilical vein endothelial cells. Mol Med Rep 15 2595 PMID: 28447716
Auvergne et al (2016) PAR1 inhibition suppresses the self-renewal and growth of A2B5-defined glioma progenitor cells and their derived gliomas in vivo. Oncogene 35 3817 PMID: 26616854
Gwairi et al (2016) Multiple Growth Factors, But Not VEGF, Stimulate Glycosaminoglycan Hyperelongation in Retinal Choroidal Endothelial Cells. Int J Biol Sci 12 1041 PMID: 27570478
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
Chen et al (2012) Thrombin activity associated with neuronal damage during acute focal ischemia. J Neurosci 32 7622 PMID: 22649241
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
Noskovičová et al (2018) Cub domain-containing protein 1 negatively regulates TGF-β signaling and myofibroblast differentiation. Am J Physiol Lung Cell Mol Physiol 314 L695 PMID: 29351434
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
Chen et al (2022) Thrombin induces morphological and inflammatory astrocytic responses via activation of PAR1 receptor. Cell Death Discov. 8 189 PMID: 35399122
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
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
Yan et al (2013) Role of SCH79797 in maintaining vascular integrity in rat model of subarachnoid hemorrhage. Nat Med 44 1410 PMID: 23539525
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
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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