MRS 2500 tetraammonium salt
Highly potent and selective antagonist of the platelet P2Y1 receptor (Ki = 0.78 nM). Inhibits ADP-induced aggregation of human platelets with an IC50 value of 0.95 nM. Inhibits the upregulation of NTPDase1 by ATPγS. Prevents thrombus formation in vivo.
Sold under license from the NIH, US Patent 10/169975
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 629.29. 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.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.59 mL||7.95 mL||15.89 mL|
|5 mM||0.32 mL||1.59 mL||3.18 mL|
|10 mM||0.16 mL||0.79 mL||1.59 mL|
|50 mM||0.03 mL||0.16 mL||0.32 mL|
References are publications that support the biological activity of the product.
Kim et al (2003) 2-Substitution of adenine nucleotide analogues containing a bicyclo[3.1.0]hexane ring system locked in a northern conformation: enhanced potency as P2Y1 receptor antagonists. J.Med.Chem 46 4974 PMID: 14584948
Cattaneo et al (2004) Antiaggregatory activity in human platelets of potent antagonists of the P2Y1 receptor. Biochem.Pharmacol. 68 1995 PMID: 15476670
Hechler et al (2006) MRS2500 [2-iodo-N6-methyl-(N)-methanocarba-2'-deoxyadenosine-3', 5'-bisphosphate], a potent, selective, and stable antagonist of the platelet P2Y1 receptor with strong antithrombotic activity in mice. J.Pharmacol.Exp.Ther. 316 556 PMID: 16236815
Lu et al (2007) Stimulation of the P2Y1 receptor up-regulates nucleoside-triphosphate diphosphohydrolase-1 in human retinal pigment epithelial cells. J.Pharmacol.Exp.Ther. 323 157 PMID: 17626796
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19 Citations for MRS 2500 tetraammonium salt
Citations are publications that use Tocris products. Selected citations for MRS 2500 tetraammonium salt include:
Liu et al (2018) Salvianolic acids from antithrombotic Traditional Chinese Medicine Danshen are antagonists of human P2Y1 and P2Y12 receptors. Sci Rep 8 11380 PMID: 30038283
Alefishat et al (2013) Antagonism of P2Y1-induced vasorelaxation by acyl CoA: a critical role for palmitate and 3'-phosphate. Br J Pharmacol 168 1911 PMID: 23215951
Fei et al (2013) Neurogenic mucosal bicarbonate secretion in guinea pig duodenum. Br J Pharmacol 168 880 PMID: 22994306
Helms et al (2013) Mechanisms of hemolysis-associated platelet activation. J Thromb Haemost 11 2148 PMID: 24119131
Ilatovskaya et al (2013) Pharmacological characterization of the P2 receptors profile in the podocytes of the freshly isolated rat glomeruli. Am J Physiol Cell Physiol 305 C1050 PMID: 24048730
Högberg et al (2009) Mild hypothermia does not attenuate platelet aggregation and may even increase ADP-stimulated platelet aggregation after clopidogrel treatment. Purinergic Signal 7 2 PMID: 19236702
Ryu et al (2017) Paradoxical induction of growth arrest and apoptosis by EGF via the up-regulation of PTEN by activating Redox factor-1/Egr-1 in human lung cancer cells. Oncotarget 8 4181 PMID: 27935858
Hwang et al (2011) β-nicotinamide adenine dinucleotide is an enteric inhibitory neurotransmitter in human and nonhuman primate colons. Gastroenterology 140 608 PMID: 20875415
Gao et al (2013) The role of P2Y(14) and other P2Y receptors in degranulation of human LAD2 mast cells. J Pharmacol Exp Ther 9 31 PMID: 22825617
Ohtani et al (2008) Evidence for the possible involvement of the P2Y(6) receptor in Ca (2+) mobilization and Ins secretion in mouse pancreatic islets. Purinergic Signal 4 365 PMID: 18784987
Baron et al (2015) The NLRP3 inflammasome is activated by nanoparticles through ATP, ADP and adenosine. Thromb J 6 e1629 PMID: 25654762
Erdélyi et al (2014) Analyzing receptor assemblies in the cell membrane using fluorescence anisotropy imaging with TIRF microscopy. PLoS One 9 e100526 PMID: 24945870
Kurahashi et al (2014) Platelet-derived growth factor receptor-α-positive cells and not smooth muscle cells mediate purinergic hyperpolarization in murine colonic muscles. Am J Physiol Cell Physiol 307 C561 PMID: 25055825
Ham et al (2010) Endogenous luminal surface adenosine signaling regulates duodenal bicarbonate secretion in rats. J Cell Biochem 335 607 PMID: 20805305
Gorman et al (2010) Adenine nucleotide control of coronary blood flow during exercise. Am J Physiol Heart Circ Physiol 299 H1981 PMID: 20852039
Braganhol et al (2015) Nucleotide receptors control IL-8/CXCL8 and MCP-1/CCL2 secretions as well as proliferation in human glioma cells. Biochim Biophys Acta 1852 120 PMID: 25445541
Duffy et al (2012) Changes in neuromuscular transmission in the W/W(v) mouse internal anal sphincter. Neurogastroenterol Motil 24 e41 PMID: 22074497
Bradley et al (2010) Novel excitatory effects of adenosine triphosphate on contractile and pacemaker activity in rabbit urethral smooth muscle. J Urol 183 801 PMID: 20022059
Konopatskaya et al (2009) PKCalpha regulates platelet granule secretion and thrombus formation in mice. J Clin Invest 119 399 PMID: 19147982
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