MRS 2578

Pricing Availability Delivery Time Qty
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 (16)
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.

All Tocris products are intended for laboratory research use only.

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
1 mM 2.12 mL 10.58 mL 21.16 mL
5 mM 0.42 mL 2.12 mL 4.23 mL
10 mM 0.21 mL 1.06 mL 2.12 mL
50 mM 0.04 mL 0.21 mL 0.42 mL

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

Product Datasheets

Certificate of Analysis / Product Datasheet
Select another batch:
Safety Datasheet

References

References are publications that support the products' biological activity.

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


If you know of a relevant reference for MRS 2578, please let us know.

View Related Products by Target

View Related Products by Product Action

View all Purinergic (P2Y) Receptor Antagonists

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

16 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

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

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

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

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

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

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

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

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


Do you know of a great paper that uses MRS 2578 from Tocris? If so please let us know.

Reviews for MRS 2578

There are currently no reviews for this product. Be the first to review MRS 2578 and earn rewards!

Have you used MRS 2578?

Submit a review and receive an Amazon gift card.

$10US/$10CAN/€7/£6 gift card for a review without an image

$25US/$25CAN/€18/£15 gift card for a review with an image

*Offer only valid in the USA / Canada, UK and Europe

Submit a Review

Literature in this Area

Cardiovascular

Cardiovascular Research Product Guide

A collection of over 250 products for cardiovascular research, the guide includes research tools for the study of:

  • Hypertension
  • Thrombosis and Hemostasis
  • Atherosclerosis
  • Myocardial Infarction
  • Ischemia/Reperfusion Injury
  • Arrhythmias
  • Heart Failure
GPCR

GPCR Product Listing

A collection of over 450 products for G protein-coupled receptors, the listing includes research tools for the study of:

  • Rhodopsin-like Receptors
  • Secretin-like Receptors
  • Glutamate Receptors
  • Frizzled Receptors
  • GPCR Signaling
Pain

Pain Research Product Guide

A collection of over 250 products for pain research, the guide includes research tools for the study of:

  • Nociception
  • Ion Channels
  • G-Protein-Coupled Receptors
  • Intracellular Signaling
P2X and P2Y Receptors

P2X and P2Y Receptors Scientific Review

Written by Kenneth Jacobson, this review provides an overview of the different subtypes and structures of the P2 receptor families, as well as the pharmacological probes used to study them; compounds available from Tocris are listed.

Cardiovascular

Cardiovascular Poster

Cardiovascular disease remains one of the major causes of morbidity and mortality in the Western world and therefore this therapeutic area continues to be of great interest to researchers. This poster highlights the key GPCRs regulating vascular reactivity.