SCH 58261
Based on 17 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.
For research use only. We do not sell to patients.
- Purity: 99.71%
- CAS No.: 160098-96-4
- Formula: C18H15N7O
- Molecular Weight:345.36
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) SCH 58261
More- Signal Transduct Target Ther. 2020 Apr 29;5(1):41. [Abstract]
- Nat Cancer. 2022 Aug;3(8):945-960. [Abstract]
- Acta Pharm Sin B. 2023 Jun;13(6):2778-2794. [Abstract]
- Int J Oral Sci. 2024 Jun 18;16(1):46. [Abstract]
- Mol Psychiatry. 2024 May 13. [Abstract]
- Acta Biomater. 2025 Apr 22:S1742-7061(25)00295-8. [Abstract]
- Anim Nutr. 2025 Jul 12.
- Antioxid Redox Signal. 2024 May 8. [Abstract]
- Talanta. 2024 May 1:271:125672. [Abstract]
- Drug Des Devel Ther. 2026 Mar 24:20:575035. [Abstract]
- Nanomedicine. 2025 Feb 3:64:102809. [Abstract]
- Molecules. 2020 May 8;25(9):2209. [Abstract]
- J Cell Commun Signal. 2024 Feb 14;18(1):e12018. [Abstract]
- Cell Signal. 2019 Jun:58:44-52. [Abstract]
- Mol Immunol. 2025 Feb 8:179:71-83. [Abstract]
- Research Square Preprint. 2024 Aug 06.
- bioRxiv. 2024 November 03.
Customer Validation & Images
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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In Vivo Efficacy Study
All Adenosine Receptor Isoforms
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Biological Activity
IC50: 15 nM (A2A receptor)[2]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CT26 | GI50 |
>100 μM
Compound: 6; SCH-58261
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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
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[PMID: 34783558] |
| MC-38 | GI50 |
>100 μM
Compound: 6; SCH-58261
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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
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[PMID: 34783558] |
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.
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Cell Line:H1975 cells
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Concentration:10 nM-10 µM
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Incubation Time:7 days
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Result:Produced a concentration-dependent decrease in H1975 cell growth.
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Cell Line:CAF cells
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Concentration:25 μM
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Incubation Time:72 hours
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Result:Inhibit the growth of CAF1 and CAF2 cells.
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.
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Animal Model:4‒6 weeks old athymic nude mice (NCI) with PC9 cells xenograft[5]
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Dosage:2 mg/kg
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Administration:Intraperitoneal injection; daily; for 20 days
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Result:Decreased tumor growth.
Chemical Information
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CAS No. 160098-96-4
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Appearance Solid
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Molecular Weight 345.36
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Formula C18H15N7O
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Color White to yellow
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SMILES
NC1=NC(N(CCC2=CC=CC=C2)N=C3)=C3C4=NC(C5=CC=CO5)=NN14
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (17)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
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).
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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 -
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 -
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.
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Mol Psychiatry
Adenosine mediates the amelioration of social novelty deficits during rhythmic light treatment of 16p11.2 deletion female mice. [Abstract]2024 May 13. PMID: 38740879 -
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 -
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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 May 8. PMID: 38717958
SCH 58261 purchased from MedChemExpress. Usage Cited in: Antioxid Redox Signal. 2024 May 8. [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 May 8. [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 May 8. [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.
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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 -
Nanomedicine
Improving lipid nanoparticles delivery efficiency of macrophage cells by using immunomodulatory small molecules. [Abstract]2025 Feb 3:64:102809. PMID: 39904398 -
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 -
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 -
Cell Signal
N4-acetylcytidine is required for sustained NLRP3 inflammasome activation via HMGB1 pathway in microglia. [Abstract]2019 Jun:58:44-52. PMID: 30853521 -
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 -
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Solvent & Solubility
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (280 KB)
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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)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[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]
Complete Stock Solution Preparation Table
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.
| 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 |
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