Home GPCR & G Protein Adenosine Receptor antagonist SCH58261 For research use only.

SCH58261

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.

SCH58261 Chemical Structure

SCH58261 Chemical Structure

CAS: 160098-96-4

Selleck's SCH58261 has been cited by 6 publications

Purity & Quality Control

Batch: Purity: 99.77%
99.77

SCH58261 Related Products

Choose Selective Adenosine Receptor Inhibitors

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293 Function assay 60 mins Displacement of [3H]CGS21680 from human adenosine A2A receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting analysis, Ki = 0.0006 μM. 23200243
CHO Function assay Displacement of [3H]-SCH- 58261 from human Adenosine A2A receptor expressed in CHO cells, Ki = 0.0011 μM. 9622554
HEK293 Function assay Displacement of specific [3H]-SCH- 58261 binding at human Adenosine A2A receptor expressed in HEK293 cells., Ki = 0.0011 μM. 11754583
CHO Function assay Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells, Ki = 0.0011 μM. 19501513
CHO Function assay 60 mins Displacement of [3H]-ZM 241385 from human adenosine A2A receptor expressed in CHO cells after 60 mins by liquid scintillation counting, Ki = 0.0011 μM. 22204739
HEK293 Function assay 60 mins Displacement of [3H]ZM241385 from human adenosine A2A receptor expressed in HEK293 cells after 60 mins by rapid filtration assay, Ki = 0.00123 μM. 20303771
HEK293 Function assay 60 mins Competitive binding affinity to human adenosine A2A receptor expressed in HEK293 cells after 60 mins by fluorescence polarization assay in presence of MRS5346, Ki = 0.0019 μM. 23200243
CHO Function assay Displacement of [3H]CHA from human Adenosine A1 receptor expressed in CHO cells, Ki = 0.549 μM. 9622554
CHO Function assay Displacement of specific [3H]DPCPX binding at human Adenosine A1 receptor expressed in CHO cells., Ki = 0.549 μM. 11754583
CHO Function assay 120 mins Displacement of [3H]-DPCPX from human adenosine A1 receptor expressed in CHO cells after 120 mins by liquid scintillation counting, Ki = 0.549 μM. 22204739
HEK293 Function assay 60 mins Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in HEK293 cells after 60 mins by rapid filtration assay, Ki = 0.5941 μM. 20303771
HEK293 Function assay Displacement of [3H]-AB MECA from human Adenosine A3 receptor expressed in HEK293 cells, Ki = 1 μM. 12646033
HEK293 Function assay Displacement of [125I]AB-MECA from human Adenosine A3 receptor expressed in HEK293 cells, Ki = 10 μM. 9622554
HEK293 Function assay Displacement of specific [3H]DPCPX binding at human adenosine A2B receptor expressed in HEK293 cells., Ki = 10 μM. 11754583
CHO Function assay Displacement of specific [3H]MRE3008-F20 binding at human adenosine A3 receptor expressed in CHO cells., Ki = 10 μM. 11754583
CHO Function assay Displacement of [3H]NECA from human adenosine A3 receptor expressed in CHO cells, Ki = 10 μM. 19501513
CHO Function assay 120 mins Displacement of [3H]-MRE-3008-F20 from human adenosine A3 receptor expressed in CHO cells after 120 mins by liquid scintillation counting, Ki = 10 μM. 22204739
HEK293 Function assay 60 mins Displacement of [3H]-DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins, Ki = 10 μM. 22204739
HEK293 Function assay 100 nM 24 hrs Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced intracellular cAMP accumulation at 100 nM after 24 hrs (Rvb= 0.40 pmol/ml) 20303771
HEK293 Function assay 1 uM 15 mins Antagonist activity at human A2A receptor expressed in HEK293 cells assessed as decrease in NECA-induced cAMP release at 1 uM after 15 mins 23953686
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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
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]
Kinase Assay 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.
In Vivo
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]
Animal Research Animal Models Mice with Spinal cord injury
Dosages 0.01 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 345.36 Formula

C18H15N7O
CAS No. 160098-96-4 SDF Download SCH58261 SDF
Smiles C1=CC=C(C=C1)CCN2C3=C(C=N2)C4=NC(=NN4C(=N3)N)C5=CC=CO5
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 69 mg/mL ( (199.79 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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