SCH 442416

Pricing Availability Delivery Time Qty
Cat.No. 2463 - SCH 442416 | C20H19N7O2 | CAS No. 316173-57-6
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)
Datasheet
Citations (6)
Literature

Biological Activity

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
Storage Store at RT
Purity ≥99% (HPLC)
CAS Number 316173-57-6
PubChem ID 10668061
InChI Key AEULVFLPCJOBCE-UHFFFAOYSA-N
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

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.

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

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

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

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 PMID:


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

6 Citations for SCH 442416

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

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

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

Ross and Venton (2015) Adenosine transiently modulates stimulated dopamine release in the caudate-putamen via A1 receptors. Exp Ther Med 132 51 PMID: 25219576

Li et al (2014) Regulation of photoreceptor gap junction phosphorylation by adenosine in zebrafish retina. Vis Neurosci 31 237 PMID: 24844306

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


Do you know of a great paper that uses SCH 442416 from Tocris? If so please let us know.

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Pathways for SCH 442416

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