MRS 2179 tetrasodium salt

Cat. No. 0900

MRS 2179 tetrasodium salt C11H13N5O9P2Na4 [1454889-37-2]

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Chemical Name: 2'-Deoxy-N6-methyladenosine 3',5'-bisphosphate tetrasodium salt

Biological Activity

A competitive antagonist at P2Y1 receptors (KB = 100 nM). Selective over P2X1 (IC50 = 1.15 μM), P2X3 (IC50 = 12.9 μM), P2X2, P2X4, P2Y2, P2Y4 and P2Y6 receptors. Inhibits the upregulation of NTPDase1 by ATPγS.

Licensing Information

Sold under license from the NIH, US Patent 60/029,855

Technical Data

Soluble to 100 mM in water
>98 %
Desiccate at -20°C

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 / Safety Data Sheet

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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.

Brown et al (2000) Activity of novel adenine nucleotide derivatives as agonists and antagonists at recombinant rat P2X receptors. Drug Dev.Res. 49 253.

Nandanan et al (2000) Synthesis, biological activity, and molecular modeling of ribose-modified deoxyadenosine bisphosphate analogues as P2Y1 receptor ligands. J.Med.Chem. 43 829. PMID: 10715151.

Boyer et al (1998) Competitive and selective antagonism of P2Y1 receptors by N6-methyl 2'-deoxyadenosine 3',5'-bisphosphate. Br.J.Pharmacol. 124 1. PMID: 9630335.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for MRS 2179 tetrasodium salt include:

Kawano et al (2015) Autocrine Regulation of UVA-Induced IL-6 Production via Release of ATP and Activation of P2Y Receptors. PLoS One 10 e0127919. PMID: 26030257.

Riquelme et al (2015) Pannexin channels mediate the acquisition of myogenic commitment in C2C12 reserve cells promoted by P2 receptor activation. J Neurosci 3 25. PMID: 26000275.

Giachini et al (2014) Anti-platelet therapy with clopidogrel prevents endothelial dysfunction and vascular remodeling in aortas from hypertensive rats. PLoS One 9 e91890. PMID: 24638017.

Tang et al (2014) Lactate-mediated glia-neuronal signalling in the mammalian brain. Nat Commun 5 3284. PMID: 24518663.

Wang et al (2014) Nucleolin down-regulation is involved in ADP-induced cell cycle arrest in S phase and cell apoptosis in vascular endothelial cells. PLoS One 9 e110101. PMID: 25290311.

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.

Ashpole et al (2013) Loss of calcium/calmodulin-dependent protein kinase II activity in cortical astrocytes decreases glutamate uptake and induces neurotoxic release of ATP. J Biol Chem 288 14599. PMID: 23543737.

Fei et al (2013) Neurogenic mucosal bicarbonate secretion in guinea pig duodenum. Br J Pharmacol 168 880. PMID: 22994306.

Oestreich et al (2013) Pharmacodynamic interplay of the P2Y(1), P2Y(12), and TxA(2) pathways in platelets: the potential of triple antiplatelet therapy with P2Y(1) receptor antagonism. Thromb Res 131 e64. PMID: 23245937.

Pinheiro et al (2013) Bradykinin-induced Ca2+ signaling in human subcutaneous fibroblasts involves ATP release via hemichannels leading to P2Y12 receptors activation. Cell Commun Signal 11 70. PMID: 24047499.

Balduini et al (2012) Constitutively released adenosine diphosphate regulates proplatelet formation by human megakaryocytes. Haematologica 97 1657. PMID: 22689668.

Begum et al (2012) DHA inhibits ER Ca2+ release and ER stress in astrocytes following in vitro ischemia. J Neurochem 120 622. PMID: 22129278.

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

Flamm et al (2012) Multiscale prediction of patient-specific platelet function under flow. Blood 120 190. PMID: 22517902.

Hazleton et al (2012) Purinergic receptors are required for HIV-1 infection of primary human macrophages. J Immunol 188 4488. PMID: 22450808.

Martín-Gil et al (2012) Silencing of P2Y(2) receptors reduces intraocular pressure in New Zealand rabbits. Br J Pharmacol 165 1163. PMID: 21740413.

Puerto et al (2012) Adenylate cyclase 5 coordinates the action of ADP, P2Y1, P2Y13 and ATP-gated P2X7 receptors on axonal elongation. J Cell Sci 125 176. PMID: 22250198.

Tran et al (2012) Dynamic mass redistribution assays decode surface influence on signaling of endogenous purinergic P2Y receptors. Assay Drug Dev Technol 10 37. PMID: 22066912.

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

Kuboyama et al (2011) Astrocytic P2Y(1) receptor is involved in the regulation of cytokine/chemokine transcription and cerebral damage in a rat model of cerebral ischemia. Front Cell Dev Biol 31 1930. PMID: 21487414.

Huang et al (2009) Autocrine and paracrine roles for ATP and serotonin in mouse taste buds. Cancer Med 29 13909. PMID: 19890001.

Li and Olson (2008) Purinergic activation of anion conductance and osmolyte efflux in cultured rat hippocampal neurons. Am J Physiol Cell Physiol 295 C1550. PMID: 18923056.

Braun et al (2007) Residual platelet ADP reactivity after clopidogrel treatment is dependent on activation of both the unblocked P2Y(1) and the P2Y (12) receptor and is correlated with protein expression of P2Y (12). Purinergic Signal 3 195. PMID: 18404433.

Mutafova-Yambolieva et al (2007) Beta-nicotinamide adenine dinucleotide is an inhibitory neurotransmitter in visceral smooth muscle. Proc Natl Acad Sci U S A 104 16359. PMID: 17913880.

Holinstat et al (2006) PAR4, but not PAR1, signals human platelet aggregation via Ca2+ mobilization and synergistic P2Y12 receptor activation. J Biol Chem 281 26665. PMID: 16837456.

Czajkowski et al (2004) Differential effects of P2Y1 and P2Y12 nucleotide receptors on ERK1/ERK2 and phosphatidylinositol 3-kinase signalling and cell proliferation in serum-deprived and nonstarved glioma C6 cells. Br J Pharmacol 141 497. PMID: 14718252.

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