SCH 442416

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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% (HPLC)
Citations (11)
Literature (1)

Biological Activity for SCH 442416

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).

Compound Libraries for SCH 442416

SCH 442416 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for SCH 442416

M. Wt 389.42
Formula C20H19N7O2
Storage Store at RT
Purity ≥99% (HPLC)
CAS Number 316173-57-6
PubChem ID 10668061
Smiles COC1=CC=C(CCCN2N=CC3=C2N=C(N)N2N=C(N=C32)C2=CC=CO2)C=C1

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.

Solubility Data for SCH 442416

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 38.94 100

Preparing Stock Solutions for SCH 442416

The following data is based on the product molecular weight 389.42. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets for SCH 442416

Certificate of Analysis / Product Datasheet
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References for SCH 442416

References are publications that support the biological activity of the product.

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

Zheng et al (2007) Protective roles of adenosine A1, A2, and A3 receptors in skeletal muscle ischemia and reperfusion injury. Am.J.Physiol.Heart Circ.Physiol. 293 3685

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Keywords: SCH 442416, SCH 442416 supplier, selective, high, affinity, A2A, antagonists, Receptors, adenosines, SCH442416, adenosine, 2a, antagonist, Adenosine, 2463, Tocris Bioscience

11 Citations for SCH 442416

Citations are publications that use Tocris products. Selected citations for SCH 442416 include:

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

Pugliese et al (2009) The adenosine A2A receptor antagonist ZM241385 enhances neuronal survival after oxygen-glucose deprivation in rat CA1 hippocampal slices. Br J Pharmacol 157 818 PMID: 19422385

Núñez et al (2018) PBF509, an Adenosine A2A Receptor Antagonist With Efficacy in Rodent Models of Movement Disorders. Front Pharmacol 9 1200 PMID: 30405415

Fang et al (2016) Expression of CD39 on activated T cells impairs their survival in older individuals. Cell Rep. 14 1218

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Literature in this Area

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