Cat. No. 2146
Chemical Name: N,N''-1,4-Butanediylbis[N'-(3-isothioc
Biological ActivitySelective 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.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
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.
Mamedova et al (2004) Diisothiocyanate derivatives as potent, insurmountable antagonists of P2Y6 nucleotide receptors. Biochem.Pharmacol. 67 1763. PMID: 15081875.
If you know of a relevant reference for MRS 2578 please let us know.
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.
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.
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.
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.
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.
Quintas et al (2014) Microglia P2Y6 receptors mediate nitric oxide release and astrocyte apoptosis. J Neuroinflammation 11 141. PMID: 25178395.
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.
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.
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.
Genetos et al (2011) Purinergic signaling is required for fluid shear stress-induced NF-κB translocation in osteoblasts. Biochem Pharmacol 317 737. PMID: 21237152.
Riegel et al (2011) Selective induction of endothelial P2Y6 nucleotide receptor promotes vascular inflammation. Blood 117 2548. PMID: 21173118.
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.
Talasila et al (2009) Characterization of P2Y receptor subtypes functionally expressed on neonatal rat cardiac myofibroblasts. Br J Pharmacol 158 339. PMID: 19422377.
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.
Kukulski et al (2007) Extracellular nucleotides mediate LPS-induced neutrophil migration in vitro and in vivo. Autophagy 81 1269. PMID: 17322022.
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Keywords: MRS 2578, supplier, Selective, P2Y6, antagonists, Receptors, Purinergic, purinoceptors, MRS2578, Tocris Bioscience, Purinergic (P2Y) Receptor Antagonist products
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