SCH79797

Additional information:
SCH-79797 is a potent and selective PAR1 antagonist. SCH-79797 limits myocardial ischemia/reperfusion injury in rat hearts. SCH 79797 protects against ischemia/reperfusion-induced arrhythmias in the rat hearts. SCH 79797 and its N-methyl analog (SCH 203099) inhibited binding of a high-affinity thrombin receptor-activating peptide ([(3)H]haTRAP, Ala-Phe(p-F)-Arg-ChA-HArg-[(3)H]Tyr-NH(2)) to PAR-1 with IC(50) values of 70 and 45 nM, respectively.|Product information|CAS Number: 245520-69-8|Molecular Weight: 371.{{Tazarotene} web|{Tazarotene} Autophagy|{Tazarotene} Biological Activity|{Tazarotene} References|{Tazarotene} custom synthesis|{Tazarotene} Epigenetic Reader Domain} 48|Formula: C23H25N5|Chemical Name: N3-cyclopropyl-7-{[4-(propan-2-yl)phenyl]methyl}-7H-pyrrolo[3, 2-f]quinazoline-1, 3-diamine|Smiles: CC(C)C1C=CC(CN2C=CC3=C4C(N)=NC(NC5CC5)=NC4=CC=C23)=CC=1|InChiKey: AVXQPEKZIGPIJW-UHFFFAOYSA-N|InChi: InChI=1S/C23H25N5/c1-14(2)16-5-3-15(4-6-16)13-28-12-11-18-20(28)10-9-19-21(18)22(24)27-23(26-19)25-17-7-8-17/h3-6,9-12,14,17H,7-8,13H2,1-2H3,(H3,24,25,26,27)|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: To be determined|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.{{Mevastatin} site|{Mevastatin} Autophagy|{Mevastatin} Technical Information|{Mevastatin} Data Sheet|{Mevastatin} manufacturer|{Mevastatin} Autophagy} |Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|SCH79797 inhibits high-affinity thrombin receptor-activating peptide ([3H]haTRAP) binding in a competitive manner. SCH79797 inhibits α-thrombin- and haTRAP-induced aggregation of human platelets, but does not inhibit human platelet aggregation induced by the tethered ligand agonist for protease-activated receptor-4 (PAR-4), γ-thrombin, ADP, or collagen. Thrombin produces transient increases in cytosolic free Ca2+ concentration ([Ca2+]i) in hCASMC. SCH79797 effectively inhibits this increase in [Ca2+]i. SCH79797 completely inhibits Thrombin- and TK-stimulated [3H]thymidine incorporation. SCH79797 is able to interfere with the growth of several human and mouse cell lines, in a concentration-dependent manner. The ED50 for growth inhibition iss 75 nM, 81 nM and 116 nM for NIH 3T3, HEK 293 and A375 cells, respectively.PMID:23664186 In NIH 3T3 cells, SCH79797 inhibits serum-stimulated activation of p44/p42 mitogen-activated protein kinases (MAPK) at low concentrations and induces apoptosis at higher concentrations.|In Vivo:|SCH79797 (2.5-250 μg/kg; intravenous injection; male Sprague Dawley rats) treatment immediately before or during ischemia reduces myocardial necrosis following I/R in the intact rat heart in two rat models of myocardial ischemia/reperfusion (I/R) injury. This response is dose-dependent with the optimal dose being 25 μg/kg.|References:|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. doi: 10.1155/2013/165453. Epub 2013 Dec 16. PubMed PMID: 24453410; PubMed Central PMCID: PMC3876890.Gong JH, Cho IH, Shin D, Han SY, Park SH, Kang YH. Inhibition of airway epithelial-to-mesenchymal transition and fibrosis by kaempferol in endotoxin-induced epithelial cells and ovalbumin-sensitized mice. Lab Invest. 2014 Mar;94(3):297-308. doi: 10.1038/labinvest.2013.137. Epub 2013 Dec 30. PubMed PMID: 24378645.Products are for research use only. Not for human use.|