MRS 2578

Catalog # Availability Size / Price Qty
2146/10
2146/50
MRS 2578 | CAS No. 711019-86-2 | P2Y Receptor Antagonists
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Description: Selective P2Y6 antagonist

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

Purity: ≥95%

Product Details
Citations (24)
Supplemental Products
Reviews (1)

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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

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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

  1. Connexin-43-dependent ATP release mediates macrophage activation during sepsis.
    Authors: Dosch Et al.
    Elife  2019;8
  2. P2Y6 Receptor-Mediated Spinal Microglial Activation in Neuropathic Pain.
    Authors: Bian Et al.
    Pain Res Manag  2019;2019:2612534
  3. Resident Macrophages Cloak Tissue Microlesions to Prevent Neutrophil-Driven Inflammatory Damage.
    Authors: Uderhardt Et al.
    Cell  2019;177:541
  4. 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
  5. 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
  6. 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
  7. 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
  8. Enhancement of glucose uptake in mouse skeletal muscle cells and adipocytes by P2Y6 receptor agonists.
    Authors: Balasubramanian Et al.
    Pharmacol Res  2014;9:e116203
  9. 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
  10. 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
  11. Microglia P2Y6 receptors mediate nitric oxide release and astrocyte apoptosis.
    Authors: Quintas Et al.
    J Neuroinflammation  2014;11:141
  12. 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
  13. 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
  14. 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
  15. Investigation of the functional expression of purine and pyrimidine receptors in porcine isolated pancreatic arteries.
    Authors: Alsaqati Et al.
    Purinergic Signal  2013;10:241
  16. 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
  17. Silencing of P2Y(2) receptors reduces intraocular pressure in New Zealand rabbits.
    Authors: Martín-Gil Et al.
    Br J Pharmacol  2012;165:1163
  18. Constitutive lysosome exocytosis releases ATP and engages P2Y receptors in human monocytes.
    Authors: Sivaramakrishnan Et al.
    J Cell Sci  2012;125:4567
  19. Purinergic signaling is required for fluid shear stress-induced NF-κB translocation in osteoblasts.
    Authors: Genetos Et al.
    Biochem Pharmacol  2011;317:737
  20. Selective induction of endothelial P2Y6 nucleotide receptor promotes vascular inflammation.
    Authors: Riegel Et al.
    Blood  2011;117:2548
  21. 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
  22. Characterization of P2Y receptor subtypes functionally expressed on neonatal rat cardiac myofibroblasts.
    Authors: Talasila Et al.
    Br J Pharmacol  2009;158:339
  23. 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
  24. Extracellular nucleotides mediate LPS-induced neutrophil migration in vitro and in vivo.
    Authors: Kukulski Et al.
    Autophagy  2007;81:1269

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MRS 2578 inhibits LPS-induced inflammation
By Anonymous on 01/22/2019
Species: Mouse

RAW macrophages were stimulated with LPS (200 ng/ml) in the absence or presence of A 804598 (1 μM) or MRS 2578 (100 μM) for 8 h to follow iNOS expression by qPCR. Both compounds inhibited LPS-induced iNOS expression revealing role of purinergic receptors.


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