MRS 2500 tetraammonium salt

Cat. No. 2159

MRS 2500 tetraammonium salt C13H18N5O8P2I.4NH3 [630103-23-0]

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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.

Licensing Information

Sold under license from the NIH, US Patent 10/169975

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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Certificate of Analysis / Product Datasheet
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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.

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.

Cattaneo et al (2004) Antiaggregatory activity in human platelets of potent antagonists of the P2Y1 receptor. Biochem.Pharmacol. 68 1995. PMID: 15476670.

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.

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

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.

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.

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.

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.

Duffy et al (2012) Changes in neuromuscular transmission in the W/W(v) mouse internal anal sphincter. Neurogastroenterol Motil 24 e41. PMID: 22074497.

Hwang et al (2011) β-nicotinamide adenine dinucleotide is an enteric inhibitory neurotransmitter in human and nonhuman primate colons. Gastroenterology 140 608. PMID: 20875415.

Gorman et al (2010) Adenine nucleotide control of coronary blood flow during exercise. Am J Physiol Heart Circ Physiol 299 H1981. PMID: 20852039.

Ham et al (2010) Endogenous luminal surface adenosine signaling regulates duodenal bicarbonate secretion in rats. J Cell Biochem 335 607. PMID: 20805305.

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.

Konopatskaya et al (2009) PKCalpha regulates platelet granule secretion and thrombus formation in mice. J Clin Invest 119 399. PMID: 19147982.

Ohtani et al (2008) Evidence for the possible involvement of the P2Y(6) receptor in Ca (2+) mobilization and insulin secretion in mouse pancreatic islets. Purinergic Signal 4 365. PMID: 18784987.

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Keywords: MRS 2500 tetraammonium salt, supplier, potent, selective, P2Y1, antagonists, Receptors, Purinergic, purinoceptors, MRS2500, prevents, thrombus, formation, Tocris Bioscience, Purinergic (P2Y) Receptor Antagonist products

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