MRS 2578

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Cat.No. 2146 - MRS 2578 | C20H20N6S4 | CAS No. 711019-86-2
Description: Selective P2Y6 antagonist
Chemical Name: N,N''-1,4-Butanediylbis[N'-(3-isothiocyanatophenyl)thiourea
Purity: ≥95% (HPLC)
Datasheet
Citations (21)
Reviews
Literature

Biological Activity

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

M. Wt 472.66
Formula C20H20N6S4
Storage Desiccate at -20°C
Purity ≥95% (HPLC)
CAS Number 711019-86-2
PubChem ID 16078986
InChI Key QOHNRGHTJPFMSL-UHFFFAOYSA-N
Smiles S=C(NCCCCNC(NC2=CC(N=C=S)=CC=C2)=S)NC1=CC(N=C=S)=CC=C1

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 Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 23.63 50

Preparing Stock Solutions

The following data is based on the product molecular weight 472.66. Batch specific molecular weights may vary from batch to batch due to solvent 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

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

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


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Keywords: MRS 2578, MRS 2578 supplier, Selective, P2Y6, antagonists, Receptors, Purinergic, purinoceptors, MRS2578, P2Y, 2146, Tocris Bioscience

21 Citations for MRS 2578

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 (2014) Enhancement of glucose uptake in mouse skeletal muscle cells and adipocytes by P2Y6 receptor agonists. Pharmacol Res 9 e116203 PMID: 25549240

Balasubramanian et al (2013) AMP-activated protein kinase as regulator of P2Y(6) receptor-induced insulin 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

Genetos et al (2011) Purinergic signaling is required for fluid shear stress-induced NF-κB translocation in osteoblasts. Biochem Pharmacol 317 737 PMID: 21237152

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

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

Kukulski et al (2007) Extracellular nucleotides mediate LPS-induced neutrophil migration in vitro and in vivo. Autophagy 81 1269 PMID: 17322022

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

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

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

Sivaramakrishnan et al (2012) Constitutive lysosome exocytosis releases ATP and engages P2Y receptors in human monocytes. J Cell Sci 125 4567 PMID: 22767503

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


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