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).
|Storage||Store at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 389.42. 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||2.57 mL||12.84 mL||25.68 mL|
|5 mM||0.51 mL||2.57 mL||5.14 mL|
|10 mM||0.26 mL||1.28 mL||2.57 mL|
|50 mM||0.05 mL||0.26 mL||0.51 mL|
References are publications that support the products' biological activity.
Todde et al (2000) 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. J.Med.Chem. 43 4359 PMID: 11087559
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Keywords: SCH 442416, supplier, selective, high, affinity, A2A, antagonists, Receptors, adenosines, SCH442416, adenosine, 2a, antagonist, Adenosine, A2A, Receptors, Adenosine, A2A, Receptors, Tocris Bioscience
6 Citations for SCH 442416
Citations are publications that use Tocris products. Selected citations for SCH 442416 include:
Yu et al (2012) 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. Am J Physiol Renal Physiol 3 803 PMID: 22969972
Varani et al (2011) A2A and A3 adenosine receptor expression in rheumatoid arthritis: upregulation, inverse correlation with disease activity score and suppression of inflammatory cytokine and metalloproteinase release. Arthritis Res Ther 13 R197 PMID: 22146575
Ross and Venton (2015) Adenosine transiently modulates stimulated dopamine release in the caudate-putamen via A1 receptors. Exp Ther Med 132 51 PMID: 25219576
Tosolini et al (2015) Human monocyte recognition of adenosine-based cyclic dinucleotides unveils the A2a Gαs protein-coupled receptor tonic inhibition of mitochondrially induced cell death. J Neurochem 35 479 PMID: 25384972
Li et al (2014) Regulation of photoreceptor gap junction phosphorylation by adenosine in zebrafish retina. Vis Neurosci 31 237 PMID: 24844306
Do you know of a great paper that uses SCH 442416 from Tocris? If so please let us know.
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