Catalog Number: 2146
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.
Background References
  1. Diisothiocyanate derivatives as potent, insurmountable antagonists of P2Y6 nucleotide receptors.
    Mamedova et al.
    Biochem.Pharmacol., 2004;67:1763
  2. UDP acting at P2Y6 receptors is a mediator of microglial phagocytosis.
    Koizumi et al.
    Nature, 2007;446:1091
  3. Extracellular nucleotides mediate LPS-induced neutrophil migration in vitro and in vivo.
    Kukulski et al.
    J.Leukoc.Biol., 2007;81:1269
Citations:

The citations listed below are publications that use Tocris products. Selected citations for MRS 2578 include:

16 Citations: Showing 1 - 10
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  1. 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
  2. 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
  3. Enhancement of glucose uptake in mouse skeletal muscle cells and adipocytes by P2Y6 receptor agonists.
    Authors: Balasubramanian Et al.
    Pharmacol Res 2014;9:e116203
  4. 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
  5. Microglia P2Y6 receptors mediate nitric oxide release and astrocyte apoptosis.
    Authors: Quintas Et al.
    J Neuroinflammation 2014;11:141
  6. 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
  7. AMP-activated protein kinase as regulator of P2Y(6) receptor-induced insulin secretion in mouse pancreatic β-cells.
    Authors: Balasubramanian Et al.
    PLoS One 2013;85:991
  8. 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
  9. 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
  10. Silencing of P2Y(2) receptors reduces intraocular pressure in New Zealand rabbits.
    Authors: Martín-Gil Et al.
    Br J Pharmacol 2012;165:1163
  11. Purinergic signaling is required for fluid shear stress-induced NF-κB translocation in osteoblasts.
    Authors: Genetos Et al.
    Biochem Pharmacol 2011;317:737
  12. Selective induction of endothelial P2Y6 nucleotide receptor promotes vascular inflammation.
    Authors: Riegel Et al.
    Blood 2011;117:2548
  13. 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
  14. Characterization of P2Y receptor subtypes functionally expressed on neonatal rat cardiac myofibroblasts.
    Authors: Talasila Et al.
    Br J Pharmacol 2009;158:339
  15. 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
  16. Extracellular nucleotides mediate LPS-induced neutrophil migration in vitro and in vivo.
    Authors: Kukulski Et al.
    Autophagy 2007;81:1269
Expand to show all 16 Citations

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