MRS 2578

Cat. No. 2146

MRS 2578 C20H20N6S4 [711019-86-2]

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Chemical Name: N,N''-1,4-Butanediylbis[N'-(3-isothiocyanatophenyl)thiourea

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
Solubility:
Soluble to 50 mM in DMSO
Purity:
>95 %
Storage:
Desiccate at -20°C
CAS No:
711019-86-2

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 / Safety Data Sheet

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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.

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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.

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.

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.

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.

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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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