MRS 2500 tetraammonium salt
Chemical Name: (1R*,2S*)-4-[2-Iodo-6-(methylamino)-9H-purin-9-yl]-2-(phosphonooxy)bicyclo[3.1.0]hexane-1-methanol dihydrogen phosphate ester tetraammonium salt
Biological ActivityHighly 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.
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.
Stimulation of the P2Y1 receptor up-regulates nucleoside-triphosphate diphosphohydrolase-1 in human retinal pigment epithelial cells.
Lu et al.
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.
Kim et al.
Antiaggregatory activity in human platelets of potent antagonists of the P2Y1 receptor.
Cattaneo et al.
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.
Hechler et al.
Citations for MRS 2500 tetraammonium salt
The citations listed below are publications that use Tocris products. Selected citations for MRS 2500 tetraammonium salt include:
20 Citations: Showing 1 - 10
Connexin-43-dependent ATP release mediates macrophage activation during sepsis.
Authors: Dosch Et al.
Salvianolic acids from antithrombotic Traditional Chinese Medicine Danshen are antagonists of human P2Y1 and P2Y12 receptors.
Authors: Liu Et al.
Sci Rep 2018;8(1):11380
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.
Authors: Ryu Et al.
The NLRP3 inflammasome is activated by nanoparticles through ATP, ADP and adenosine.
Authors: Baron Et al.
Thromb J 2015;6:e1629
Nucleotide receptors control IL-8/CXCL8 and MCP-1/CCL2 secretions as well as proliferation in human glioma cells.
Authors: Braganhol Et al.
Biochim Biophys Acta 2015;1852:120
Analyzing receptor assemblies in the cell membrane using fluorescence anisotropy imaging with TIRF microscopy.
Authors: Erdélyi Et al.
PLoS One 2014;9:e100526
Platelet-derived growth factor receptor-α-positive cells and not smooth muscle cells mediate purinergic hyperpolarization in murine colonic muscles.
Authors: Kurahashi Et al.
Am J Physiol Cell Physiol 2014;307:C561
The role of P2Y(14) and other P2Y receptors in degranulation of human LAD2 mast cells.
Authors: Gao Et al.
J Pharmacol Exp Ther 2013;9:31
Pharmacological characterization of the P2 receptors profile in the podocytes of the freshly isolated rat glomeruli.
Authors: Ilatovskaya Et al.
Am J Physiol Cell Physiol 2013;305:C1050
Neurogenic mucosal bicarbonate secretion in guinea pig duodenum.
Authors: Fei Et al.
Br J Pharmacol 2013;168:880
Antagonism of P2Y1-induced vasorelaxation by acyl CoA: a critical role for palmitate and 3'-phosphate.
Authors: Alefishat Et al.
Br J Pharmacol 2013;168:1911
Mechanisms of hemolysis-associated platelet activation.
Authors: Helms Et al.
J Thromb Haemost 2013;11:2148
Changes in neuromuscular transmission in the W/W(v) mouse internal anal sphincter.
Authors: Duffy Et al.
Neurogastroenterol Motil 2012;24:e41
β-nicotinamide adenine dinucleotide is an enteric inhibitory neurotransmitter in human and nonhuman primate colons.
Authors: Hwang Et al.
Endogenous luminal surface adenosine signaling regulates duodenal bicarbonate secretion in rats.
Authors: Ham Et al.
J Cell Biochem 2010;335:607
Adenine nucleotide control of coronary blood flow during exercise.
Authors: Gorman Et al.
Am J Physiol Heart Circ Physiol 2010;299:H1981
Novel excitatory effects of adenosine triphosphate on contractile and pacemaker activity in rabbit urethral smooth muscle.
Authors: Bradley Et al.
J Urol 2010;183:801
Mild hypothermia does not attenuate platelet aggregation and may even increase ADP-stimulated platelet aggregation after clopid. treatment.
Authors: Högberg Et al.
Purinergic Signal 2009;7:2
PKCalpha regulates platelet granule secretion and thrombus formation in mice.
Authors: Konopatskaya Et al.
J Clin Invest 2009;119:399
Evidence for the possible involvement of the P2Y(6) receptor in Ca (2+) mobilization and Ins secretion in mouse pancreatic islets.
Authors: Ohtani Et al.
Purinergic Signal 2008;4:365
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