Catalog Number: 2159
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 Activity
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.
Technical Data
  • M.Wt:
    629.29
  • Formula:
    C13H18N5O8P2I.4NH3
  • Solubility:
    Soluble to 100 mM in water
  • Purity:
    >96%
  • Storage:
    Store at -20°C
  • CAS No:
    630103-23-0
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Additional Information
Licensing Caveats:
Sold under license from the NIH, US Patent 10/169975
Background References
  1. Stimulation of the P2Y1 receptor up-regulates nucleoside-triphosphate diphosphohydrolase-1 in human retinal pigment epithelial cells.
    Lu et al.
    J.Pharmacol.Exp.Ther., 2007;323:157
  2. 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.
    J.Med.Chem, 2003;46:4974
  3. Antiaggregatory activity in human platelets of potent antagonists of the P2Y1 receptor.
    Cattaneo et al.
    Biochem.Pharmacol., 2004;68:1995
  4. 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.
    J.Pharmacol.Exp.Ther., 2006;316:556
Citations:

The citations listed below are publications that use Tocris products. Selected citations for MRS 2500 tetraammonium salt include:

15 Citations: Showing 1 - 10
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  1. The NLRP3 inflammasome is activated by nanoparticles through ATP, ADP and adenosine.
    Authors: Baron Et al.
    Thromb J 2015;6:e1629
  2. Analyzing receptor assemblies in the cell membrane using fluorescence anisotropy imaging with TIRF microscopy.
    Authors: Erdélyi Et al.
    PLoS One 2014;9:e100526
  3. 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
  4. 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
  5. 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
  6. Neurogenic mucosal bicarbonate secretion in guinea pig duodenum.
    Authors: Fei Et al.
    Br J Pharmacol 2013;168:880
  7. 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
  8. Mechanisms of hemolysis-associated platelet activation.
    Authors: Helms Et al.
    J Thromb Haemost 2013;11:2148
  9. Changes in neuromuscular transmission in the W/W(v) mouse internal anal sphincter.
    Authors: Duffy Et al.
    Neurogastroenterol Motil 2012;24:e41
  10. β-nicotinamide adenine dinucleotide is an enteric inhibitory neurotransmitter in human and nonhuman primate colons.
    Authors: Hwang Et al.
    Gastroenterology 2011;140:608
  11. Endogenous luminal surface adenosine signaling regulates duodenal bicarbonate secretion in rats.
    Authors: Ham Et al.
    J Cell Biochem 2010;335:607
  12. Adenine nucleotide control of coronary blood flow during exercise.
    Authors: Gorman Et al.
    Am J Physiol Heart Circ Physiol 2010;299:H1981
  13. Mild hypothermia does not attenuate platelet aggregation and may even increase ADP-stimulated platelet aggregation after clopidogrel treatment.
    Authors: Högberg Et al.
    Purinergic Signal 2009;7:2
  14. PKCalpha regulates platelet granule secretion and thrombus formation in mice.
    Authors: Konopatskaya Et al.
    J Clin Invest 2009;119:399
  15. Evidence for the possible involvement of the P2Y(6) receptor in Ca (2+) mobilization and insulin secretion in mouse pancreatic islets.
    Authors: Ohtani Et al.
    Purinergic Signal 2008;4:365
Expand to show all 15 Citations

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