MRS 2179 tetrasodium salt

Name: MRS 2179 tetrasodium salt
Brand: Tocris Bioscience
SKU: 0900
Rating: 5 (1 reviews)

Tocris Bioscience a Bio-Techne Brand

Catalog # 0900

Citations (35)

(1)

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Key Product Details

Description:	Selective P2Y₁ antagonist
Chemical Name:	2'-Deoxy-N⁶-methyladenosine 3',5'-bisphosphate tetrasodium salt
Purity:	≥98% (HPLC)
Molecular Weight:	513.16

View Full Technical Details for MRS 2179 tetrasodium salt

Biological Activity for MRS 2179 tetrasodium salt

MRS 2179 tetrasodium salt is a competitive antagonist at P2Y₁ receptors (K_B = 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.

Technical Data for MRS 2179 tetrasodium salt

M. Wt	513.16
Formula	C₁₁H₁₃N₅O₉P₂Na₄
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	1454889-37-2
PubChem ID	90479745
InChi Key	XLPQPYQWGFCKEY-IDAKGYGSSA-J
Smiles	[Na+].[Na+].[Na+].[Na+].CNC1=NC=NC2=C1N=CN2[C@@H]1C[C@H](OP([O-])([O-])=O)[C@@H](COP([O-])([O-])=O)O1

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 2179 tetrasodium salt

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	water	25.66	50

Preparing Stock Solutions for MRS 2179 tetrasodium salt

The following data is based on the product molecular weight 513.16.

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
0.5 mM	3.90 mL	19.49 mL	38.97 mL
2.5 mM	0.78 mL	3.90 mL	7.79 mL
5 mM	0.39 mL	1.95 mL	3.90 mL
25 mM	0.08 mL	0.39 mL	0.78 mL

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References for MRS 2179 tetrasodium 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
Nandanan Synthesis, biological activity, and molecular modeling of ribose-modified deoxyadenosine bisphosphate analogues as P2Y₁ receptor ligands. J.Med.Chem. 2000 PMID: 10715151
Brown Activity of novel adenine nucleotide derivatives as agonists and antagonists at recombinant rat P2X receptors. Drug Dev.Res. 2000 PMID: 22791931
Nandanan Structure-activity relationships of bisphosphate nucleotide derivatives as P2Y₁ receptor antagonists and partial agonists. J.Med.Chem. 1999 PMID: 10229631
Boyer Competitive and selective antagonism of P2Y₁ receptors by N⁶-methyl 2'-deoxyadenosine 3',5'-bisphosphate. Br.J.Pharmacol. 1998 PMID: 9630335

Citations for MRS 2179 tetrasodium salt (35)

Showing 1 - 10 of 35 citations Showing All

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

Ng (2018) Inhibition of cytokine-mediated JNK signalling by purinergic P2Y11 receptors, a novel protective mechanism in endothelial cells. Cell Signal. 51:59
PMID: 30076967
Barría et al. (2018) Trypanosoma cruzi Infection Induces Pannexin-1 Channel Opening in Cardiac Myocytes. Am J Trop Med Hyg. 98:105
PMID: 29141748
Kleiner et al. (2018) Activator protein-1 contributes to the NaCl-induced expression of VEGF and PlGF in RPE cells. Mol Vis. 24:647
PMID: 30310263
Makkawi (2017) A complementary role for tetraspanin superfamily member TSSC6 and ADP purinergic P2Y12 receptor in platelets. Thromb Res. 161:12
PMID: 29178985
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
Liñán-Rico et al. (2015) Neuropharmacology of purinergic receptors in human submucous plexus: Involvement of P2X1, P2X2, P2X3 channels, P2Y and A3 metabotropic receptors in neurotransmission. Neuropharmacology. 95:83
PMID: 25724083
Tang et al. (2014) Lactate-mediated glia-neuronal signalling in the mammalian brain. Nat Commun. 5:3284
PMID: 24518663
Giachini et al. (2014) Anti-platelet therapy with clopid. prevents endothelial dysfunction and vascular remodeling in aortas from hypertensive rats. PLoS One. 9:e91890
PMID: 24638017
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
Li and Diamond (2014) Detection of platelet sensitivity to inhibitors of COX-1, P2Y1, and P2Y12 using a whole blood microfluidic flow assay. Thromb Res. 133:203
PMID: 24365044
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
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
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
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
Alsaqati et al. (2013) Investigation of the functional expression of purine and pyrimidine receptors in porcine isolated pancreatic arteries. Purinergic Signal. 10:241
PMID: 24310605
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
Duffy et al. (2012) Changes in neuromuscular transmission in the W/W(v) mouse internal anal sphincter. Neurogastroenterol Motil. 24:e41
PMID: 22074497
Begum et al. (2012) DHA inhibits ER Ca²⁺ release and ER stress in astrocytes following in vitro ischemia. J Neurochem. 120:622
PMID: 22129278
Flamm et al. (2012) Multiscale prediction of patient-specific platelet function under flow. Blood. 120:190
PMID: 22517902
Martín-Gil et al. (2012) Silencing of P2Y(2) receptors reduces intraocular pressure in New Zealand rabbits. Br J Pharmacol. 165:1163
PMID: 21740413
Hazleton et al. (2012) Purinergic receptors are required for HIV-1 infection of primary human macrophages. J Immunol. 188:4488
PMID: 22450808
Balduini et al. (2012) Constitutively released adenosine diphosphate regulates proplatelet formation by human megakaryocytes. Haematologica. 97:1657
PMID: 22689668
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
Chandaka et al. (2011) Facilitation of transmitter release from rat sympathetic neurons via presynaptic P2Y(1) receptors. Br J Pharmacol. 164:1522
PMID: 21557728
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
Gallego et al. (2008) Purinergic and nitrergic junction potential in the human colon. Am J Physiol Gastrointest Liver Physiol. 295:G522
PMID: 18599588
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
Braun et al. (2007) Residual platelet ADP reactivity after clopid. 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
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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works well

Name: Karthik krishnamurthy

Species: Mouse

Assay Type: In Vitro

Cell Line/Tissue: astrocytes

used to block P2Y1 receptor mediated calcium entry in mouse astrocytes stimulated with 2MeSADP

25 micromolar of MRS2179 was bath applied.

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Product Documents for MRS 2179 tetrasodium salt

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Certificate of Analysis

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