Tozadenant [870070-55-6]

Referência HY-10995-50mg

Tamanho : 50mg

Marca : MedChemExpress

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Tozadenant is an adenosine A2A receptor antagonist, with Ki of 11.5 nM on human A2A and 6 nM on rhesus A2A.

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Tozadenant Chemical Structure

Tozadenant Chemical Structure

CAS No. : 870070-55-6

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Based on 4 publication(s) in Google Scholar

    Tozadenant purchased from MedChemExpress. Usage Cited in: PLoS One. 2016 Nov 11;11(11):e0166415.  [Abstract]

    The endogenous Aβ production of SH-SY5Y cells upon the treatment with 0.1% of DMSO (Vehicle), Istradefylline (Istrad.), Preladenant (Prelad.) or Tozadenant (Tozad.) at 30 nM for 24 h is examined.

    Voir tous les produits spécifiques à Isoform Adenosine Receptor:

    Voir toutes les isoformes
    Adenosine A1 receptor (A1R) Adenosine A2A receptor (A2AR) Adenosine A2B receptor (A2BR) Adenosine A3 receptor (A3R)
    Description

    Tozadenant is an adenosine A2A receptor antagonist, with Ki of 11.5 nM on human A2A and 6 nM on rhesus A2A.

    IC50 & Target

    Ki: 6 nM (Rhesus A2A), 11.5 nM (Human A2A)

    In Vivo

    18F-MNI-444 regional uptake is consistent with A2A receptor distribution in the brain. Selectivity is demonstrated by dose-dependent blocking by tozadenant (1.5, 10.5 mg/kg) and preladenant[1].

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

    Essai clinique
    Masse moléculaire

    406.50

    Formule

    C19H26N4O4S

    CAS No.

    870070-55-6

    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(NC1=NC2=C(C=CC(N3CCOCC3)=C2S1)OC)N4CCC(O)(CC4)C

    Livraison

    Room temperature in continental US; may vary elsewhere.

    Stockage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvant et solubilité
    In Vitro: 

    DMSO : 50 mg/mL (123.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.4600 mL 12.3001 mL 24.6002 mL
    5 mM 0.4920 mL 2.4600 mL 4.9200 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.

    • Calculateur de molarité

    • Calculateur de dilution

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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: ≥ 2.5 mg/mL (6.15 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (6.15 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    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.
    Pureté et documentation

    Purity: 98.30%

    Références
    • [1]. Olivier Barret, et al. Adenosine 2A Receptor Occupancy by Tozadenant and Preladenant in Rhesus Monkeys. J Nucl Med. 2014 Oct;55(10):1712-8.  [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 2.4600 mL 12.3001 mL 24.6002 mL 61.5006 mL
    5 mM 0.4920 mL 2.4600 mL 4.9200 mL 12.3001 mL
    10 mM 0.2460 mL 1.2300 mL 2.4600 mL 6.1501 mL
    15 mM 0.1640 mL 0.8200 mL 1.6400 mL 4.1000 mL
    20 mM 0.1230 mL 0.6150 mL 1.2300 mL 3.0750 mL
    25 mM 0.0984 mL 0.4920 mL 0.9840 mL 2.4600 mL
    30 mM 0.0820 mL 0.4100 mL 0.8200 mL 2.0500 mL
    40 mM 0.0615 mL 0.3075 mL 0.6150 mL 1.5375 mL
    50 mM 0.0492 mL 0.2460 mL 0.4920 mL 1.2300 mL
    60 mM 0.0410 mL 0.2050 mL 0.4100 mL 1.0250 mL
    80 mM 0.0308 mL 0.1538 mL 0.3075 mL 0.7688 mL
    100 mM 0.0246 mL 0.1230 mL 0.2460 mL 0.6150 mL
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    Tozadenant Related Classifications

    Help & FAQs

    Keywords:

    Tozadenant870070-55-6SYN115SYN 115SYN-115Adenosine ReceptorP1 receptorInhibitorinhibitorinhibit

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