Home / Adenosine A2a Receptor Antagonists / SCH 442416

SCH 442416

Catalog #: 2463
11 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
2463/10
2463/50
2463/1
SCH 442416 | CAS No. 316173-57-6 | Adenosine A2a Receptor Antagonists
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Description: Very selective, high affinity A2A antagonist

Chemical Name: 2-(2-Furanyl)-7-[3-(4-methoxyphenyl)propyl]-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine

Purity: ≥99%

Product Details
Citations (11)
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Biological Activity

SCH 442416 is a selective adenosine A2A receptor antagonist; binds to human and rat A2A receptors with high affinity (Ki values are 0.048 and 0.5 nM respectively). Displays > 23000-fold selectivity for hA2A over hA1 in vitro with minimal affinity for hA2B and hA3 receptors (IC50 > 10 μM). Blocks the cytoprotective effect of A2A agonist CGS-21680 (Cat.No. 1063).

Technical Data

M.Wt:
389.42
Formula:
C20H19N7O2
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥99%
Storage:
Store at RT
CAS No:
316173-57-6

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.

Background References

  1. Multiple sclerosis lymphocytes upregulate A2A adenosine receptors that are antiinflammatory when stimulated.
    Vincenzi F, Corciulo C, Targa M, Merighi S, Gessi S, Casetta I, Gentile M, Granieri E, Borea P, Varani K
    Eur J Immunol, 2013;43(8):2206-16.
  2. Role and Function of A2A and A? Adenosine Receptors in Patients with Ankylosing Spondylitis, Psoriatic Arthritis and Rheumatoid Arthritis
    A Ravani, F Vincenzi, A Bortoluzzi, M Padovan, S Pasquini, S Gessi, S Merighi, PA Borea, M Govoni, K Varani
    Int J Mol Sci, 2017;18(4):.
  3. Human monocyte recognition of adenosine-based cyclic dinucleotides unveils the A2a Galphas protein-coupled receptor tonic inhibition of mitochondrially induced cell death.
    Tosolini M, Pont F, Betous D, Ravet E, Ligat L, Lopez F, Poupot M, Poirot M, Perouzel E, Tiraby G, Verhoeyen E, Fournie J
    Mol Cell Biol, 2015;35(2):479-95.
  4. Design, radiosynthesis, and biodistribution of a new potent and selective ligand for in vivo imaging of the adenosine A2A receptor system using positron emission tomography.
    Todde et al.
    J.Med.Chem., 2000;43:4359
  5. Protective roles of adenosine A1, A2, and A3 receptors in skeletal muscle ischemia and reperfusion injury.
    Zheng et al.
    Am.J.Physiol.Heart Circ.Physiol., 2007;293:3685

Product Datasheets

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Citations for SCH 442416

The citations listed below are publications that use Tocris products. Selected citations for SCH 442416 include:

11 Citations: Showing 1 - 10

  1. PBF509, an Adenosine A2A Receptor Antagonist With Efficacy in Rodent Models of Movement Disorders.
    Authors: Núñez Et al.
    Front Pharmacol  2018;9:1200
  2. Structures of Human A1 and A2A Adenosine Receptors with Xanthines Reveal Determinants of Selectivity.
    Authors: Cheng Et al.
    Structure  2017;25:1275
  3. Expression of CD39 on Activated T Cells Impairs their Survival in Older Individuals.
    Authors: Fang Et al.
    Cell Rep  2016;14:1218
  4. Expression of CD39 on activated T cells impairs their survival in older individuals.
    Authors: Fang Et al.
    Cell Rep.  2016;14:1218
  5. Human monocyte recognition of adenosine-based cyclic dinucleotides unveils the A2a Gαs protein-coupled receptor tonic inhibition of mitochondrially induced cell death.
    Authors: Tosolini Et al.
    J Neurochem  2015;35:479
  6. Adenosine transiently modulates stimulated DA release in the caudate-putamen via A1 receptors.
    Authors: Ross and Venton
    Exp Ther Med  2015;132:51
  7. Regulation of photoreceptor gap junction phosphorylation by adenosine in zebrafish retina.
    Authors: Li Et al.
    Vis Neurosci  2014;31:237
  8. Cardiac myocyte-secreted cAMP exerts paracrine action via adenosine receptor activation.
    Authors: Sassi Et al.
    J Clin Invest  2014;124:5385
  9. Effect of A(2A) receptor antagonist (SCH 442416) on the mRNA expression of glutamate aspartate transporter and glutamine synthetase in rat retinal Müller cells under hypoxic conditions in vitro.
    Authors: Yu Et al.
    Am J Physiol Renal Physiol  2012;3:803
  10. A2A and A3 adenosine receptor expression in rheumatoid arthritis: upregulation, inverse correlation with disease activity score and suppression of inflammatory cytokine and metalloproteinase release.
    Authors: Varani Et al.
    Arthritis Res Ther  2011;13:R197

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