MRS 2578
Chemical Name: N,N''-1,4-Butanediylbis[N'-(3-isothiocyanatophenyl)thiourea
Purity: ≥95%
Biological Activity
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.Technical Data
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
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Enhancement of glucose uptake in mouse skeletal muscle cells and adipocytes by P2Y6 receptor agonists.
Balasubramanian R, Robaye B, Boeynaems J, Jacobson K
PLoS ONE, 2014;9(12):e116203. -
Tumour necrosis factor alpha-induced neuronal loss is mediated by microglial phagocytosis.
Neniskyte U, Vilalta A, Brown G
FEBS Lett, 2014;588(17):2952-6. -
Extracellular nucleotides mediate LPS-induced neutrophil migration in vitro and in vivo.
Kukulski et al.
J.Leukoc.Biol., 2007;81:1269 -
Diisothiocyanate derivatives as potent, insurmountable antagonists of P2Y6 nucleotide receptors.
Mamedova et al.
Biochem.Pharmacol., 2004;67:1763 -
UDP acting at P2Y6 receptors is a mediator of microglial phagocytosis.
Koizumi et al.
Nature, 2007;446:1091
Product Datasheets
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Citations for MRS 2578
The citations listed below are publications that use Tocris products. Selected citations for MRS 2578 include:
24 Citations: Showing 1 - 10
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Connexin-43-dependent ATP release mediates macrophage activation during sepsis.
Authors: Dosch Et al.
Elife 2019;8
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P2Y6 Receptor-Mediated Spinal Microglial Activation in Neuropathic Pain.
Authors: Bian Et al.
Pain Res Manag 2019;2019:2612534
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Resident Macrophages Cloak Tissue Microlesions to Prevent Neutrophil-Driven Inflammatory Damage.
Authors: Uderhardt Et al.
Cell 2019;177:541
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Nucleotide receptors control IL-8/CXCL8 and MCP-1/CCL2 secretions as well as proliferation in human glioma cells.
Authors: Braganhol Et al.
Biochim Biophys Acta 2015;1852:120
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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.
Authors: Nishimura Et al.
PLoS Pathog 2015;11:e1005184
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The PRKAA1/AMPKα1 pathway triggers autophagy during CSF1-induced human monocyte differentiation and is a potential target in CMML.
Authors: Obba Et al.
Exp Cell Res 2015;11:1114
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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
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Enhancement of glucose uptake in mouse skeletal muscle cells and adipocytes by P2Y6 receptor agonists.
Authors: Balasubramanian Et al.
Pharmacol Res 2014;9:e116203
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Activation of P2Y6 receptors increases the voiding frequency in anaesthetized rats by releasing ATP from the bladder urothelium.
Authors: Carneiro Et al.
Br J Pharmacol 2014;171:3404
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P2Y6 receptor inhibition perturbs CCL2-evoked signalling in human monocytic and peripheral blood mononuclear cells.
Authors: Campwala Et al.
J Cell Sci 2014;127:4964
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Microglia P2Y6 receptors mediate nitric oxide release and astrocyte apoptosis.
Authors: Quintas Et al.
J Neuroinflammation 2014;11:141
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Role of spinal P2Y6 and P2Y11 receptors in neuropathic pain in rats: possible involvement of glial cells.
Authors: Barragán-Iglesias Et al.
Mol Pain 2014;10:29
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AMP-activated protein kinase as regulator of P2Y(6) receptor-induced Ins secretion in mouse pancreatic β-cells.
Authors: Balasubramanian Et al.
PLoS One 2013;85:991
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Extracellular UDP enhances P2X-mediated bladder smooth muscle contractility via P2Y(6) activation of the phospholipase C/inositol trisphosphate pathway.
Authors: Yu Et al.
FASEB J 2013;27:1895
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Investigation of the functional expression of purine and pyrimidine receptors in porcine isolated pancreatic arteries.
Authors: Alsaqati Et al.
Purinergic Signal 2013;10:241
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Pharmacological characterization of uracil nucleotide-preferring P2Y receptors modulating intestinal motility: a study on mouse ileum.
Authors: Zizzo Et al.
Purinergic Signal 2012;8:275
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Silencing of P2Y(2) receptors reduces intraocular pressure in New Zealand rabbits.
Authors: Martín-Gil Et al.
Br J Pharmacol 2012;165:1163
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Constitutive lysosome exocytosis releases ATP and engages P2Y receptors in human monocytes.
Authors: Sivaramakrishnan Et al.
J Cell Sci 2012;125:4567
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Purinergic signaling is required for fluid shear stress-induced NF-κB translocation in osteoblasts.
Authors: Genetos Et al.
Biochem Pharmacol 2011;317:737
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Selective induction of endothelial P2Y6 nucleotide receptor promotes vascular inflammation.
Authors: Riegel Et al.
Blood 2011;117:2548
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Involvement of SLC17A9-dependent vesicular exocytosis in the mechanism of ATP release during T cell activation.
Authors: Tokunaga Et al.
J Biol Chem 2010;285:17406
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Characterization of P2Y receptor subtypes functionally expressed on neonatal rat cardiac myofibroblasts.
Authors: Talasila Et al.
Br J Pharmacol 2009;158:339
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Attenuation of apoptosis in vitro and ischemia/reperfusion injury in vivo in mouse skeletal muscle by P2Y6 receptor activation.
Authors: Mamedova Et al.
Transl Oncol 2008;58:232
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Extracellular nucleotides mediate LPS-induced neutrophil migration in vitro and in vivo.
Authors: Kukulski Et al.
Autophagy 2007;81:1269
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