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MRS 2578 is a selective antagonist of P2Y6 nucleotide receptors; IC50 values are 37 and 98 nM at human and rat P2Y6 receptors respectively. Displays no activity at P2Y1, P2Y2, P2Y4 and P2Y11 receptors (IC50 > 10 μM). Inhibits agonist-induced cardiomyocyte contraction and UDP-induced phagocytosis.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 472.66. 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||4.23 mL||21.16 mL||42.31 mL|
|2.5 mM||0.85 mL||4.23 mL||8.46 mL|
|5 mM||0.42 mL||2.12 mL||4.23 mL|
|25 mM||0.08 mL||0.42 mL||0.85 mL|
References are publications that support the biological activity of the product.
Mamedova et al (2004) Diisothiocyanate derivatives as potent, insurmountable antagonists of P2Y6 nucleotide receptors. Biochem.Pharmacol. 67 1763 PMID: 15081875
Koizumi et al (2007) UDP acting at P2Y6 receptors is a mediator of microglial phagocytosis. Nature 446 1091 PMID: 17410128
Kukulski et al (2007) Extracellular nucleotides mediate LPS-induced neutrophil migration in vitro and in vivo. J.Leukoc.Biol. 81 1269 PMID: 17322022
If you know of a relevant reference for MRS 2578, please let us know.
Keywords: MRS 2578, MRS 2578 supplier, Selective, P2Y6, antagonists, Receptors, Purinergic, purinoceptors, MRS2578, antagonises, inhibitors, inhibits, P2Y, 2146, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for MRS 2578 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
Balasubramanian et al (2013) AMP-activated protein kinase as regulator of P2Y(6) receptor-induced Ins secretion in mouse pancreatic β-cells. PLoS One 85 991 PMID: 23333427
Riegel et al (2011) Selective induction of endothelial P2Y6 nucleotide receptor promotes vascular inflammation. Blood 117 2548 PMID: 21173118
Mamedova et al (2008) Attenuation of apoptosis in vitro and ischemia/reperfusion injury in vivo in mouse skeletal muscle by P2Y6 receptor activation. Transl Oncol 58 232 PMID: 18805489
Barragán-Iglesias et al (2014) Role of spinal P2Y6 and P2Y11 receptors in neuropathic pain in rats: possible involvement of glial cells. Mol Pain 10 29 PMID: 24886406
Quintas et al (2014) Microglia P2Y6 receptors mediate nitric oxide release and astrocyte apoptosis. J Neuroinflammation 11 141 PMID: 25178395
Campwala et al (2014) P2Y6 receptor inhibition perturbs CCL2-evoked signalling in human monocytic and peripheral blood mononuclear cells. J Cell Sci 127 4964 PMID: 25271060
Genetos et al (2011) Purinergic signaling is required for fluid shear stress-induced NF-κB translocation in osteoblasts. Biochem Pharmacol 317 737 PMID: 21237152
Uderhardt et al (2019) Resident Macrophages Cloak Tissue Microlesions to Prevent Neutrophil-Driven Inflammatory Damage. Cell 177 541 PMID: 30955887
Kukulski et al (2007) Extracellular nucleotides mediate LPS-induced neutrophil migration in vitro and in vivo. Autophagy 81 1269 PMID: 17322022
Bian et al (2019) P2Y6 Receptor-Mediated Spinal Microglial Activation in Neuropathic Pain. Pain Res Manag 2019 2612534 PMID: 31281556
Obba et al (2015) The PRKAA1/AMPKα1 pathway triggers autophagy during CSF1-induced human monocyte differentiation and is a potential target in CMML. Exp Cell Res 11 1114 PMID: 26029847
Carneiro et al (2014) Activation of P2Y6 receptors increases the voiding frequency in anaesthetized rats by releasing ATP from the bladder urothelium. Br J Pharmacol 171 3404 PMID: 24697602
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
Martín-Gil et al (2012) Silencing of P2Y(2) receptors reduces intraocular pressure in New Zealand rabbits. Br J Pharmacol 165 1163 PMID: 21740413
Zizzo et al (2012) Pharmacological characterization of uracil nucleotide-preferring P2Y receptors modulating intestinal motility: a study on mouse ileum. Purinergic Signal 8 275 PMID: 22102167
Tokunaga et al (2010) Involvement of SLC17A9-dependent vesicular exocytosis in the mechanism of ATP release during T cell activation. J Biol Chem 285 17406 PMID: 20382737
Dosch et al (2019) Connexin-43-dependent ATP release mediates macrophage activation during sepsis. Elife 8 PMID: 30735126
Sivaramakrishnan et al (2012) Constitutive lysosome exocytosis releases ATP and engages P2Y receptors in human monocytes. J Cell Sci 125 4567 PMID: 22767503
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
Nishimura et al (2015) The Suramin Derivative NF449 Interacts with the 5-fold Vertex of the Enterovirus A71 Capsid to Prevent Virus Attachment to PSGL-1 and Heparan Sulfate. PLoS Pathog 11 e1005184 PMID: 26430888
Yu et al (2013) Extracellular UDP enhances P2X-mediated bladder smooth muscle contractility via P2Y(6) activation of the phospholipase C/inositol trisphosphate pathway. FASEB J 27 1895 PMID: 23362118
Talasila et al (2009) Characterization of P2Y receptor subtypes functionally expressed on neonatal rat cardiac myofibroblasts. Br J Pharmacol 158 339 PMID: 19422377
Balasubramanian et al (2014) Enhancement of glucose uptake in mouse skeletal muscle cells and adipocytes by P2Y6 receptor agonists. Pharmacol Res 9 e116203 PMID: 25549240
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DMSO dilution 10 μM
RAW macrophages were stimulated with LPS (200 ng/ml) in the absence or presence of A 804598 (1 μM) or MRS 2578 (100 μM) for 8 h to follow iNOS expression by qPCR. Both compounds inhibited LPS-induced iNOS expression revealing role of purinergic receptors.
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