2. GPCR/G Protein
  3. Adenosine Receptor
  4. SCH 58261

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.

CAS No. : 160098-96-4

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Customer Review

Based on 17 publication(s) in Google Scholar

Other Forms of SCH 58261:

SCH 58261 Related Antibodies

Top Publications Citing Use of Products

    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.

    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.

    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).

    View All Adenosine Receptor Isoform Specific Products:

    View All Isoforms
    Adenosine A1 receptor (A1R) Adenosine A2A receptor (A2AR) Adenosine A2B receptor (A2BR) Adenosine A3 receptor (A3R)

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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[1][2][3].

    IC50 & Target

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

    SCH 58261 Related Antibodies

    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.
    Molecular Weight

    345.36

    Formula

    C18H15N7O
    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    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.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.8955 mL 14.4776 mL 28.9553 mL
    5 mM 0.5791 mL 2.8955 mL 5.7911 mL
    View the 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.

    • Molarity Calculator

    • Dilution Calculator

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

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    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.

    • 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.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • 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

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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

    Purity: 99.71%

    SDS (393 KB)

    COA (248 KB) LCMS (120 KB)

    Handling Instructions (2659 KB)
    References

    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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    SCH 58261 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    SCH 58261160098-96-4SCH58261SCH-58261Adenosine ReceptorP1 receptorInhibitorinhibitorinhibit

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