MRS 2500 tetraammonium salt

Name: MRS 2500 tetraammonium salt
Brand: Tocris Bioscience
SKU: 2159

Catalog # 2159 | Tocris Bioscience a Bio-Techne Brand

Citations (22)

COA / SDS

Highly potent and selective P2Y1 antagonist

Key Product Details

Description:	Highly potent and selective P2Y₁ antagonist
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
Purity:	≥96% (HPLC)
Molecular Weight:	629.29

View Full Technical Details for MRS 2500 tetraammonium salt

Technical Data
Citations (22) / Reviews

Biological Activity for MRS 2500 tetraammonium salt

MRS 2500 tetraammonium salt is a highly potent and selective antagonist of the platelet P2Y₁ receptor (K_i = 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 for MRS 2500 tetraammonium salt

M. Wt	629.29
Formula	C₁₃H₁₈N₅O₈P₂I.4NH₃
Storage	Store at -20°C
Purity	≥96% (HPLC)
CAS Number	630103-23-0
PubChem ID	90488745
InChi Key	FVTFHHDVLNQSME-AVAGOIHISA-N
Smiles	IC4=NC1=C(C(NC)=N4)N=CN1[C@H]2C[C@H](OP(O)(O)=O)[C@@]3(COP(O)(O)=O)[C@@H]2C3.N.N.N.N

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.

Solubility for MRS 2500 tetraammonium salt

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	water	12.59	20

Preparing Stock Solutions for MRS 2500 tetraammonium salt

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
0.2 mM	7.95 mL	39.73 mL	79.45 mL
1 mM	1.59 mL	7.95 mL	15.89 mL
2 mM	0.79 mL	3.97 mL	7.95 mL
10 mM	0.16 mL	0.79 mL	1.59 mL

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References for MRS 2500 tetraammonium salt

References are publications that support the biological activity of the product.

Lu Stimulation of the P2Y₁ receptor up-regulates nucleoside-triphosphate diphosphohydrolase-1 in human retinal pigment epithelial cells. J.Pharmacol.Exp.Ther. 2007 PMID: 17626796
Hechler 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. 2006 PMID: 16236815
Cattaneo Antiaggregatory activity in human platelets of potent antagonists of the P2Y₁ receptor. Biochem.Pharmacol. 2004 PMID: 15476670
Kim 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 2003 PMID: 14584948

Citations for MRS 2500 tetraammonium salt (22)

Showing 1 - 10 of 22 citations Showing All

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

Babola et al. (2021) Purinergic signaling controls spontaneous activity in the auditory system throughout early development. J.Neurosci.. 41:594
PMID: 33303678
Babola et al. (2020) Purinergic signaling in cochlear supporting cells reduces hair cell excitability by increasing the extracellular space. Elife. 9:e52160
PMID: 31913121
Dosch et al. (2019) Connexin-43-dependent ATP release mediates macrophage activation during sepsis. Elife. 8
PMID: 30735126
Liu et al. (2018) Salvianolic acids from antithrombotic Traditional Chinese Medicine Danshen are antagonists of human P2Y1 and P2Y12 receptors. Sci Rep. 8(1):11380
PMID: 30038283
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
Baron et al. (2015) The NLRP3 inflammasome is activated by nanoparticles through ATP, ADP and adenosine. Thromb J. 6:e1629
PMID: 25654762
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
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
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
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
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
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
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
Högberg et al. (2009) Mild hypothermia does not attenuate platelet aggregation and may even increase ADP-stimulated platelet aggregation after clopid. treatment. Purinergic Signal. 7:2
PMID: 19236702
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

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