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MRS 2179 tetrasodium salt

Catalog #: 0900
35 Citations Datasheet / COA / SDS
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0900/10
0900/50
MRS 2179 tetrasodium salt | CAS No. 1454889-37-2 | P2Y Receptor Antagonists
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Description: Selective P2Y1 antagonist

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

Purity: ≥98%

Product Details
Citations (35)
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Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

MRS 2179 tetrasodium salt is 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.

Technical Data

M.Wt:
513.16
Formula:
C11H13N5O9P2Na4
Solubility:
Soluble to 50 mM in water
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
1454889-37-2

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.

Background References

  1. Beta-arrestin-1 participates in thrombosis and regulates integrin aIIbbeta3 signalling without affecting P2Y receptors desensitisation and function.
    Schaff M, Receveur N, Bourdon C, Ohlmann P, Lanza F, Gachet C, Mangin PH
    Thromb. Haemost., 2012;107(4):735-48.
  2. Multiscale prediction of patient-specific platelet function under flow.

    Blood, 2012;120(0):190-198.
  3. Activation of neuronal P2X7 receptor-pannexin-1 mediates death of enteric neurons during colitis.
    Gulbransen BD, Bashashati M, Hirota SA
    Nat. Med., 2012;18(4):600-4.
  4. Purinergic receptors are required for HIV-1 infection of primary human macrophages.
    Hazleton JE, Berman JW, Eugenin EA
    J. Immunol., 2012;188(9):4488-95.
  5. 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
  6. Synthesis, biological activity, and molecular modeling of ribose-modified deoxyadenosine bisphosphate analogues as P2Y1 receptor ligands.
    Nandanan et al.
    J.Med.Chem., 2000;43:829
  7. Competitive and selective antagonism of P2Y1 receptors by N6-methyl 2'-deoxyadenosine 3',5'-bisphosphate.
    Boyer et al.
    Br.J.Pharmacol., 1998;124:1
  8. Structure-activity relationships of bisphosphate nucleotide derivatives as P2Y1 receptor antagonists and partial agonists.
    Nandanan et al.
    J.Med.Chem., 1999;42:1625
  9. Activity of novel adenine nucleotide derivatives as agonists and antagonists at recombinant rat P2X receptors.
    Brown et al.
    Drug Dev.Res., 2000;49:253

Product Datasheets

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Citations for MRS 2179 tetrasodium salt

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

35 Citations: Showing 1 - 10

  1. Trypanosoma cruzi Infection Induces Pannexin-1 Channel Opening in Cardiac Myocytes.
    Authors: Barría Et al.
    Am J Trop Med Hyg  2018;98:105
  2. Inhibition of cytokine-mediated JNK signalling by purinergic P2Y11 receptors, a novel protective mechanism in endothelial cells.
    Authors: Ng
    Cell Signal  2018;51:59
  3. Activator protein-1 contributes to the NaCl-induced expression of VEGF and PlGF in RPE cells.
    Authors: Kleiner Et al.
    Mol Vis  2018;24:647
  4. A complementary role for tetraspanin superfamily member TSSC6 and ADP purinergic P2Y12 receptor in platelets.
    Authors: Makkawi
    Thromb Res  2017;161:12
  5. Neuropharmacology of purinergic receptors in human submucous plexus: Involvement of P2X1, P2X2, P2X3 channels, P2Y and A3 metabotropic receptors in neurotransmission.
    Authors: Liñán-Rico Et al.
    Neuropharmacology  2015;95:83
  6. Pannexin channels mediate the acquisition of myogenic commitment in C2C12 reserve cells promoted by P2 receptor activation.
    Authors: Riquelme Et al.
    J Neurosci  2015;3:25
  7. Autocrine Regulation of UVA-Induced IL-6 Production via Release of ATP and Activation of P2Y Receptors.
    Authors: Kawano Et al.
    PLoS One  2015;10:e0127919
  8. Anti-platelet therapy with clopid. prevents endothelial dysfunction and vascular remodeling in aortas from hypertensive rats.
    Authors: Giachini Et al.
    PLoS One  2014;9:e91890
  9. Nucleolin down-regulation is involved in ADP-induced cell cycle arrest in S phase and cell apoptosis in vascular endothelial cells.
    Authors: Wang Et al.
    PLoS One  2014;9:e110101
  10. Lactate-mediated glia-neuronal signalling in the mammalian brain.
    Authors: Tang Et al.
    Nat Commun  2014;5:3284
  11. Detection of platelet sensitivity to inhibitors of COX-1, P2Y1, and P2Y12 using a whole blood microfluidic flow assay.
    Authors: Li and Diamond
    Thromb Res  2014;133:203
  12. Loss of calcium/calmodulin-dependent protein kinase II activity in cortical astrocytes decreases glutamate uptake and induces neurotoxic release of ATP.
    Authors: Ashpole Et al.
    J Biol Chem  2013;288:14599
  13. Neurogenic mucosal bicarbonate secretion in guinea pig duodenum.
    Authors: Fei Et al.
    Br J Pharmacol  2013;168:880
  14. 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
  15. 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.
    Authors: Oestreich Et al.
    Thromb Res  2013;131:e64
  16. Bradykinin-induced Ca2+ signaling in human subcutaneous fibroblasts involves ATP release via hemichannels leading to P2Y12 receptors activation.
    Authors: Pinheiro Et al.
    Cell Commun Signal  2013;11:70
  17. Investigation of the functional expression of purine and pyrimidine receptors in porcine isolated pancreatic arteries.
    Authors: Alsaqati Et al.
    Purinergic Signal  2013;10:241
  18. Constitutively released adenosine diphosphate regulates proplatelet formation by human megakaryocytes.
    Authors: Balduini Et al.
    Haematologica  2012;97:1657
  19. Changes in neuromuscular transmission in the W/W(v) mouse internal anal sphincter.
    Authors: Duffy Et al.
    Neurogastroenterol Motil  2012;24:e41
  20. Purinergic receptors are required for HIV-1 infection of primary human macrophages.
    Authors: Hazleton Et al.
    J Immunol  2012;188:4488
  21. Silencing of P2Y(2) receptors reduces intraocular pressure in New Zealand rabbits.
    Authors: Martín-Gil Et al.
    Br J Pharmacol  2012;165:1163
  22. Adenylate cyclase 5 coordinates the action of ADP, P2Y1, P2Y13 and ATP-gated P2X7 receptors on axonal elongation.
    Authors: Puerto Et al.
    J Cell Sci  2012;125:176
  23. DHA inhibits ER Ca2+ release and ER stress in astrocytes following in vitro ischemia.
    Authors: Begum Et al.
    J Neurochem  2012;120:622
  24. Multiscale prediction of patient-specific platelet function under flow.
    Authors: Flamm Et al.
    Blood  2012;120:190
  25. Dynamic mass redistribution assays decode surface influence on signaling of endogenous purinergic P2Y receptors.
    Authors: Tran Et al.
    Assay Drug Dev Technol  2012;10:37
  26. Astrocytic P2Y(1) receptor is involved in the regulation of cytokine/chemokine transcription and cerebral damage in a rat model of cerebral ischemia.
    Authors: Kuboyama Et al.
    Front Cell Dev Biol  2011;31:1930
  27. Facilitation of transmitter release from rat sympathetic neurons via presynaptic P2Y(1) receptors.
    Authors: Chandaka Et al.
    Br J Pharmacol  2011;164:1522
  28. β-nicotinamide adenine dinucleotide is an enteric inhibitory neurotransmitter in human and nonhuman primate colons.
    Authors: Hwang Et al.
    Gastroenterology  2011;140:608
  29. Autocrine and paracrine roles for ATP and serotonin in mouse taste buds.
    Authors: Huang Et al.
    Cancer Med  2009;29:13909
  30. Purinergic and nitrergic junction potential in the human colon.
    Authors: Gallego Et al.
    Am J Physiol Gastrointest Liver Physiol  2008;295:G522
  31. Purinergic activation of anion conductance and osmolyte efflux in cultured rat hippocampal neurons.
    Authors: Li and Olson
    Am J Physiol Cell Physiol  2008;295:C1550
  32. 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).
    Authors: Braun Et al.
    Purinergic Signal  2007;3:195
  33. Beta-nicotinamide adenine dinucleotide is an inhibitory neurotransmitter in visceral smooth muscle.
    Authors: Mutafova-Yambolieva Et al.
    Proc Natl Acad Sci U S A  2007;104:16359
  34. PAR4, but not PAR1, signals human platelet aggregation via Ca2+ mobilization and synergistic P2Y12 receptor activation.
    Authors: Holinstat Et al.
    J Biol Chem  2006;281:26665
  35. 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.
    Authors: Czajkowski Et al.
    Br J Pharmacol  2004;141:497

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