Art. -Nr.: HY-19533

SCH 58261

Name: SCH 58261
Brand: MedChemExpress
SKU: HY-19533
Price: 96.00 USD
Availability: InStock
Rating: 5 (18 reviews)

18 Cited Publications

Kundenbewertung

Based on 18 publication(s) in Google Scholar

SCH 58261 is a potent, selective and competitive antagonist of adenosine A2A receptor with an IC₅₀ of 15 nM, and displays 323-, 53- and 100-fold more selective for A2A receptor than A1, A2B, and A3 receptors, respectively.

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Reinheit: 99.71%
CAS. Nr.: 160098-96-4
Formel: C₁₈H₁₅N₇O
Molecular Weight:345.36

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

SCH 58261 Chemical Structure

CAS. Nr.: 160098-96-4

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (18)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 15 nM (A2A receptor)^[2]

Alle Adenosine Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CT26	GI₅₀	>100 μM Compound: 6; SCH-58261	Antiproliferative activity against mouse CT26 cells measured after 72 hrs by CCK8 assay Antiproliferative activity against mouse CT26 cells measured after 72 hrs by CCK8 assay	[PMID: 34783558]
MC-38	GI₅₀	>100 μM Compound: 6; SCH-58261	Antiproliferative activity against mouse MC38 cells measured after 72 hrs by CCK8 assay Antiproliferative activity against mouse MC38 cells measured after 72 hrs by CCK8 assay	[PMID: 34783558]

In Vitro

SCH 58261 (0 nM–10 μM; 7 days) decreases cell viability in a concentration-dependent in the NSCLC cell line H1975^[4].
SCH58261 (25 μM; 72 hours) can inhibit the growth of CAF cells^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[4]

Cell Line:

H1975 cells
Concentration:

10 nM-10 µM
Incubation Time:

7 days
Result:

Produced a concentration-dependent decrease in H1975 cell growth.

Cell Proliferation Assay^[5]

Cell Line:

CAF cells
Concentration:

25 μM
Incubation Time:

72 hours
Result:

Inhibit the growth of CAF1 and CAF2 cells.

In Vivo

SCH 58261 (2 mg/kg; i.p.; daily; for 20 days) causes a decrease in the tumor burden in a NSCLC mouse model^[5].
SCH 58261 (5 mg/kg; i.p.; 3 times; every 3 hours; 10 minutes before haloperidol) partially decreases the haloperidol-induced catalepsy and the increase in the PENK mRNA expression in both dorsolateral and ventrolateral parts of the striatum at all three examined levels^[6].
SCH 58261 diminishes the parkinsonian-like muscle rigidity and potentiates the effect of L-DOPA in rat model^[7].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

4‒6 weeks old athymic nude mice (NCI) with PC9 cells xenograft^[5]
Dosage:

2 mg/kg
Administration:

Intraperitoneal injection; daily; for 20 days
Result:

Decreased tumor growth.

Chemical Information

CAS. Nr. 160098-96-4
Appearance Solid
Molecular Weight 345.36
Formel C₁₈H₁₅N₇O
Color White to yellow
SMILES

NC1=NC(N(CCC2=CC=CC=C2)N=C3)=C3C4=NC(C5=CC=CO5)=NN14
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (18)

All Cell Proliferation/Viability AssayWBIn Vivo Efficacy StudyIF

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Journal Impact Factor

Signal Transduct Target Ther

Breast cancer-derived exosomes transmit lncRNA SNHG16 to induce CD73+γδ1 Treg cells. [Abstract]

2020 Apr 29;5(1):41. PMID: 32345959

SCH 58261 purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2020 Apr 29;5(1):41. [Abstract]

SCH 58261 (0.1 mM; 6 days) inhibited CD3+ T-cell proliferation. CFSE-labelled CD3+ T cells cultured in the presence or absence of A2A (SCH 58261; 0.1 mM) or A2B (PSB603) antagonists and then co-cultured with CD3+CD73+Vδ1 T cells isolated from breast tumour tissue. CD3+ T-cell proliferation was evaluated on day 6 by flow cytometry. The bar chart summarises the ratio of proliferating CD3+ T cells (CFSElow).
Nat Cancer

Cancer-associated fibroblasts employ NUFIP1-dependent autophagy to secrete nucleosides and support pancreatic tumor growth. [Abstract]

2022 Aug;3(8):945-960. PMID: 35982178
Int J Oral Sci

Nociceptive adenosine A2A receptor on trigeminal nerves orchestrates CGRP release to regulate the progression of oral squamous cell carcinoma. [Abstract]

2024 Jun 18;16(1):46. PMID: 38886342

SCH 58261 purchased from MedChemExpress. Usage Cited in: Int J Oral Sci. 2024 Jun 18;16(1):46. [Abstract]

SCH 58261 (SCH58261; 5 mg/kg; ip) reversed the phosphorylation of CREB in trigeminal ganglia (TG) in Male BALB/c nu/nu mice aged 6 weeks. Phosphorylation of CREB and total CREB in the trigeminal ganglia of healthy mice, mice carrying HSC3 tumor xenograft, and tumor-bearing mice treated with 5 mg/kg SCH58261 for 3 h.

SCH 58261 purchased from MedChemExpress. Usage Cited in: Int J Oral Sci. 2024 Jun 18;16(1):46. [Abstract]

In vivo growth of HSC3 xenograft in nontreated mice and those treated with SCH 58261 (SCH58261; 5 mg/kg; ip; daily for 18 days), n = 6 mice. (Left panel) Representative HE images of HSC3 xenografts in mice treated with vehicle or 5 mg/kg SCH58261 (Right panel).

SCH 58261 purchased from MedChemExpress. Usage Cited in: Int J Oral Sci. 2024 Jun 18;16(1):46. [Abstract]

SCH 58261 (SCH58261; 5 mg/kg; ip; daily for 18 days) showed the CGRP signal did not alter in TRPV1+ nerves surrounding tumor xenograft (Fig.a, b), yet significantly enhanced in intra-tumoral nociceptors(Fig. a, c).

SCH 58261 purchased from MedChemExpress. Usage Cited in: Int J Oral Sci. 2024 Jun 18;16(1):46. [Abstract]

SCH 58261 (SCH58261; 5 mg/kg; ip; daily for 18 days) significantly decreased the level of circulating CGRP in tumor-bearing mice.
Acta Pharm Sin B

Bone-derived MSCs encapsulated in alginate hydrogel prevent collagen-induced arthritis in mice through the activation of adenosine A2A/2B receptors in tolerogenic dendritic cells. [Abstract]

2023 Jun;13(6):2778-2794. PMID: 37425054
Acta Biomater

Immune-activated microspheres for enhanced chemoembolization of hepatocellular carcinoma by blocking the adenosine A2A receptor. [Abstract]

2025 Apr 22:S1742-7061(25)00295-8. PMID: 40274057
Mol Psychiatry

Adenosine mediates the amelioration of social novelty deficits during rhythmic light treatment of 16p11.2 deletion female mice. [Abstract]

2024 Nov;29(11):3381-3394. PMID: 38740879
Anim Nutr

2025 Jul 12.
Antioxid Redox Signal

Adenosine A2A receptor antagonist SCH58261 improves the cognitive function in Alzheimer's disease model mice through activation of Nrf2 via an autophagy-dependent pathway. [Abstract]

2024 Dec;41(16-18):1117-1133. PMID: 38717958

SCH 58261 purchased from MedChemExpress. Usage Cited in: Antioxid Redox Signal. 2024 Dec;41(16-18):1117-1133. [Abstract]

SCH 58261 (SCH; 50 mg/kg/day for 21 continuous days, i.p.) ameliorated cognitive deficits in Aβ1–42-induced AD mouse model. Effects of SCH (i.p) on the total distance (A), number of central entries (B), and time spent in central area (C) of mice in the open-field test. Effects of SCH on the discrimination index of mice in the novel object recognition test (D). Effects of SCH on the latency (E) and number of errors (F) of mice in the passive avoidance test.

SCH 58261 purchased from MedChemExpress. Usage Cited in: Antioxid Redox Signal. 2024 Dec;41(16-18):1117-1133. [Abstract]

SCH 58261 (SCH; 50 mg/kg/day for 21 continuous days, i.p.) showed A2AR protein expression was significantly increased in the Aβ1–42 group, with no change after SCH treatment in the cortex.

SCH 58261 purchased from MedChemExpress. Usage Cited in: Antioxid Redox Signal. 2024 Dec;41(16-18):1117-1133. [Abstract]

SCH 58261 (SCH; 50 mg/kg/day for 21 continuous days, i.p.) showed A2AR protein expression was significantly increased in the Aβ1–42 group, with no change after SCH treatment in the cortex.
Talanta

Programmable stopped-flow injection analysis: A comparative study on the effects of adenosine and its aptamer on respiratory burst of salivary and circulatory neutrophils. [Abstract]

2024 May 1:271:125672. PMID: 38295446
Drug Des Devel Ther

Cordycepin Ameliorates Dextran Sulfate Sodium-Induced Ulcerative Colitis in Mice by Inhibiting IL-6/IL-6R-Mediated p38 MAPK and NF-κB Activation Through Adenosine A2A Receptor Stimulation. [Abstract]

2026 Mar 24:20:575035. PMID: 41908945
Int J Mol Sci

Adenosine A2A Receptor Contributes to Bidirectional Remodeling of Microglial Inflammatory Responses During Methamphetamine Exposure. [Abstract]

2026 Jun 4;27(11):5072. PMID: 42278596
Molecules

Assessment of Pharmacokinetics and Metabolism Profiles of SCH 58261 in Rats Using Liquid Chromatography-Mass Spectrometric Method. [Abstract]

2020 May 8;25(9):2209. PMID: 32397307
Cell Signal

N4-acetylcytidine is required for sustained NLRP3 inflammasome activation via HMGB1 pathway in microglia. [Abstract]

2019 Jun:58:44-52. PMID: 30853521
Nanomedicine

Improving lipid nanoparticles delivery efficiency of macrophage cells by using immunomodulatory small molecules. [Abstract]

2025 Feb:64:102809. PMID: 39904398
J Cell Commun Signal

Lactate drives CD38 signaling to promote Epithelial-Mesenchymal Transition through Snail induction in non-small cell lung cancer cells. [Abstract]

2024 Feb 14;18(1):e12018. PMID: 38545257
Mol Immunol

Human placental mesenchymal stem cells regulate the antioxidant capacity of CD8+PD-1+ T cells through the CD73/ADO/Nrf2 pathway to protect against liver damage in mice with acute graft-versus-host disease. [Abstract]

2025 Feb 8:179:71-83. PMID: 39923662
Research Square Preprint

2024 Aug 06.
bioRxiv

2024 November 03.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 34 mg/mL (98.45 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.8955 mL

14.4776 mL

28.9553 mL

5 mM

0.5791 mL

2.8955 mL

5.7911 mL

10 mM

0.2896 mL

1.4478 mL

2.8955 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (6.02 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (6.02 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Zocchi C, et al. Binding of the radioligand [3H]-SCH 58261, a new non-xanthine A2A adenosine receptor antagonist, to rat striatal membranes. Br J Pharmacol. 1996 Apr;117(7):1381-6. [Content Brief]

[2]. Varani K, et al. Pharmacological and biochemical characterization of purified A2a adenosine receptors in human platelet membranes by [3H]-CGS 21680 binding. Br J Pharmacol. 1996 Apr;117(8):1693-701. [Content Brief]

[3]. Xi J, et al. Adenosine A2A and A2B receptors work in concert to induce a strong protection against reperfusion injury in rat hearts. J Mol Cell Cardiol. 2009 Nov;47(5):684-90. [Content Brief]

[4]. Kuzumaki N, et al. Multiple analyses of G-protein coupled receptor (GPCR) expression in the development of gefitinib-resistance in transforming non-small-cell lung cancer. PLoS One. 2012;7(10):e44368. [Content Brief]

[5]. Mediavilla-Varela M, et al. Antagonism of adenosine A2A receptor expressed by lung adenocarcinoma tumor cells and cancer associated fibroblasts inhibits their growth. Cancer Biol Ther. 2013 Sep;14(9):860-8. [Content Brief]

[6]. Wardas J, et al. SCH 58261, a selective adenosine A2A receptor antagonist, decreases the haloperidol-enhanced proenkephalin mRNA expression in the rat striatum. Brain Res. 2003 Jul 11;977(2):270-7. [Content Brief]

[7]. Wardas J, et al. SCH 58261, an A(2A) adenosine receptor antagonist, counteracts parkinsonian-like muscle rigidity in rats. Synapse. 2001 Aug;41(2):160-71. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.8955 mL	14.4776 mL	28.9553 mL	72.3882 mL
	5 mM	0.5791 mL	2.8955 mL	5.7911 mL	14.4776 mL
	10 mM	0.2896 mL	1.4478 mL	2.8955 mL	7.2388 mL
	15 mM	0.1930 mL	0.9652 mL	1.9304 mL	4.8259 mL
	20 mM	0.1448 mL	0.7239 mL	1.4478 mL	3.6194 mL
	25 mM	0.1158 mL	0.5791 mL	1.1582 mL	2.8955 mL
	30 mM	0.0965 mL	0.4826 mL	0.9652 mL	2.4129 mL
	40 mM	0.0724 mL	0.3619 mL	0.7239 mL	1.8097 mL
	50 mM	0.0579 mL	0.2896 mL	0.5791 mL	1.4478 mL
	60 mM	0.0483 mL	0.2413 mL	0.4826 mL	1.2065 mL
	80 mM	0.0362 mL	0.1810 mL	0.3619 mL	0.9049 mL

Bioz

Keywords

SCH 58261

18 Cited Publications

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SCH 58261

CGS 21680 Hydrochloride

ZM241385

DPCPX

Adenosine

5'-N-Ethylcarboxamidoadenosine

PSB-603

Inosine

Forskolin

Istradefylline

MRS 1754

MRS 1523

Sodium metatungstate

Publications Citing Use of MedChemExpress (MCE) SCH 58261

Alle Adenosine Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (18)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Bioz

SCH 58261

CGS 21680 Hydrochloride

ZM241385

DPCPX

Adenosine

5'-N-Ethylcarboxamidoadenosine

PSB-603

Inosine

Forskolin

Istradefylline

MRS 1754

MRS 1523

Sodium metatungstate

Publications Citing Use of MedChemExpress (MCE) SCH 58261

Alle Adenosine Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (18)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SCH 58261 Related Classifications

HY-19533 Related Classifications

Bioz