SCH58261

Catalog No.S8104 Batch:S810402

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Technical Data

Formula

C18H15N7O
Molecular Weight 345.36 CAS No. 160098-96-4
Solubility (25°C)* In vitro DMSO 69 mg/mL (199.79 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
0.4mg/ml Taking the 1 mL working solution as an example, add 50 μL of 8 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
1.15mg/ml Taking the 1 mL working solution as an example, add 50 μL of 23 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description SCH 58261 is a potent and selective A2a adenosine receptor antagonist with Ki of 2.3 nM and 2 nM for rat A2a and bovine A2a, respectively.
Targets
bovine A2a [1] rat A2a [1]
2.0 nM(Ki) 2.3 nM(Ki)
In vitro

SCH 58261 causes the inhibition of rabbit platelet aggregation and porcine coronary artery relaxation by antagonizing competitively the effects induced by CGS 21680. [1]
In vivo

In mice with Spinal cord injury, SCH58261 (0.01 mg/kg, i.p.) reduces demyelination and levels of TNF-α, Fas-L, PAR, Bax expression and activation of JNK MAPK. Chronic SCH58261 administration improves the neurological deficit up. [2]

In rats with 6-OHDA-induced Parkinson's disease, SCH58261 (2 mg/kg, i.p.) improves the 6-OHDA-induced bradykinesia and motor disturbance. [3]

Protocol (from reference)

Kinase Assay:

[1]
  • Receptor binding assay

    Rat brain tissues (cortex and striatum) are obtained from male Sprague-Dawley rats weighing 250 to 300 g. Bovine brain tissues (frontal cortex and striatum) are obtained from a local abattoir within 10 mm from animal sacrifice. A1 and A2a ADO receptor binding assays are performed using [3H]CHA and [3H]CGS 21680 [3H]2-[4-(2-carboxyethyl)-phenethylamino]- 5’-N-ethylcarboxamidoadenosinel as radioligands, respectively. Binding assay to CHO cells stably transfected with the rat brain A3 ADO receptor is performed using [125I]AB-MECA as radioligand. In order to determine the type of inhibition (competitive or noncompetitive), saturation experiments at A1 ADO ([3H]CHA, 0.125-64 nM) and A2a ADO receptors ([3HJCGS 21680, 1-128 aM) are carried out on rat brain tissues in the absence or in the presence of different concentrations of SCH 58261 (7-(2-phenylethyl)-5-amino-2-(2-furyl)-pyrazolo-[4,3-e]-1,2,4- triazolo[1,5-c]pyrimidine}. The affinity of SCH 58261 for several neurotransmitter binding sites, such as alpha-1, alpha-2 and beta-1 adrenoceptors, D1 and D2 dopamine receptors, 5-HT1 and 5-HT2 receptors, M1 and M2 muscarinic receptors, mu-opioid, benzodiazepine and N-methyl-D-aspartate receptors, is measured according to standard methods.
Animal Study:

[2]
  • Animal Models

    Mice with Spinal cord injury

  • Dosages

    0.01 mg/kg

  • Administration

    i.p.

Selleck's SCH58261 has been cited by 7 publications

Astrocytes in preoptic area regulate acute nociception-induced hypothermia through adenosine receptors [ CNS Neurosci Ther, 2024, 30(5):e14726] PubMed: 38715251
Adenosine A2A Receptor Antagonist Improves Cognitive Impairment by Inhibiting Neuroinflammation and Excitatory Neurotoxicity in Chronic Periodontitis Mice [ Molecules, 2022, 27(19)6267] PubMed: 36234803
The adenosine A2A receptor alleviates postoperative delirium-like behaviors by restoring blood cerebrospinal barrier permeability in rats [ J Neurochem, 2021, 10.1111/jnc.15436] PubMed: 34033116
Electroacupuncture improves neuronal plasticity through the A2AR/cAMP/PKA signaling pathway in SNL rats [ Neurochem Int, 2021, 145:104983] PubMed: 33577869
Targeting of the A2A adenosine receptor counteracts immunosuppression in vivo in a mouse model of chronic lymphocytic leukemia. [ Haematologica, 2020, 16 pii: haematol] PubMed: 32299906
Neuronal mechanisms of adenosine A 2A receptors in the loss of consciousness induced by propofol general anesthesia with functional magnetic resonance imaging (fMRI) [ J Neurochem, 2020, 10.1111/jnc.15146] PubMed: 32785947
Adenosine Receptor A1-A2a Heteromers Regulate EAAT2 Expression and Glutamate Uptake via YY1-Induced Repression of PPARγ Transcription. [ PPAR Res, 2020, 2020:2410264] PubMed: 32206061

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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