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SCH58261

Name: SCH58261
Brand: Selleck Chemicals
SKU: S8104
Rating: 5 (7 reviews)

Catalog No.S8104 Purity:99.77%

SCH 58261 is a potent and selective A2a adenosine receptor antagonist with K_i of 2.3 nM and 2 nM for rat A2a and bovine A2a, respectively.

SCH58261 Chemical Structure

CAS No. 160098-96-4

Purity & Quality Control

Batch: Purity: 99.77%

99.77

SCH58261 Related Products

Related Targets	Adenosine A1 receptor	Click to Expand
Related Products	Reversine CGS 21680 HCl ZM241385 A2AR antagonist 1 Ciforadenant (CPI-444) Imaradenant (AZD4635)	Click to Expand
Related Compound Libraries	FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Bioactive Compound Library-Ⅱ GPCR Compound Library	Click to Expand

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	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
Click to View More Cell Line Experimental Data

Biological Activity

Description

SCH 58261 is a potent and selective A2a adenosine receptor antagonist with K_i 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
Kinase 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.

References

[4] Hou X, et al. PPAR Res. 2020 Mar 6;2020:2410264.

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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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.					In vivo Formulation Calculator
	Clear solution	5% DMSO 1 95% Corn oil	0.4mg/ml (1.16mM)	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.	In vivo Formulation Calculator
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	1.15mg/ml (3.33mM)	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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	1.15mg/ml (3.33mM)	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.
Clear solution	4%DMSO 1 40%PEG300 2 4%Tween80 3 52%ddH2O	2.0mg/ml (5.79mM)	Taking the 1 mL working solution as an example, add 40 μL of 50 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 40 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 520 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
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