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  3. Clozapine N-oxide dihydrochloride

Clozapine N-oxide dihydrochloride 

Cat. No.: HY-17366A Purity: 99.97%
COA Handling Instructions

Clozapine N-oxide dihydrochloride is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide dihydrochloride activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide dihydrochloride can cross the blood-brain barrier. Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC50=11 nM) agonist.

For research use only. We do not sell to patients.

Clozapine N-oxide dihydrochloride Chemical Structure

Clozapine N-oxide dihydrochloride Chemical Structure

CAS No. : 2250025-93-3

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10 mM * 1 mL in DMSO
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Customer Review

Based on 69 publication(s) in Google Scholar

Other Forms of Clozapine N-oxide dihydrochloride:

Top Publications Citing Use of Products

68 Publications Citing Use of MCE Clozapine N-oxide dihydrochloride

IF

    Clozapine N-oxide dihydrochloride purchased from MedChemExpress. Usage Cited in: Biol Psychiatry. 2017 May 1;81(9):737-747.  [Abstract]

    c-fos immunoreactivity in the VTA 90 minutes after injections of 1 mg/kg Clozapine N-oxide (CNO).

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Clozapine N-oxide dihydrochloride is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide dihydrochloride activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide dihydrochloride can cross the blood-brain barrier[1][2][3][4]. Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC50=11 nM) agonist[5][6].

    IC50 & Target

    mAChR3

     

    mAChR4

     

    In Vitro

    Clozapine N-oxide (CNO) can bind to non-DREADD receptors at concentrations required for DREADD activation, and undergoes reverse-metabolism to its parent compound clozapine, an atypical antipsychotic that acts at a variety of pharmacological targets and produces numerous physiological and behavioral effects[2].

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

    In Vivo

    After a single intraperitoneal (i.p.) injection of Clozapine N-oxide (1 mg/kg) into mice, Clozapine N-oxide (CNO) plasma levels peak at 15 min and are very low after 2 h. Despite the short plasma half-life of CNO in mice, the biological effects that have been described after acute treatment of DREADD-expressing experimental animals are usually much longer (6-10 h)[1].

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

    Molecular Weight

    415.74

    Formula

    C18H21Cl3N4O

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    C[N+]1([O-])CCN(C2=NC3=CC(Cl)=CC=C3NC4=CC=CC=C42)CC1.[H]Cl.[H]Cl

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, stored under nitrogen

    *In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)

    Solvent & Solubility
    In Vitro: 

    DMSO : 240 mg/mL (577.28 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 100 mg/mL (240.53 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.4053 mL 12.0267 mL 24.0535 mL
    5 mM 0.4811 mL 2.4053 mL 4.8107 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, 1 year; -20°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • 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)

    C1

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    Volume (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: ≥ 6 mg/mL (14.43 mM); Clear solution

      This protocol yields a clear solution of ≥ 6 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (60.0 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: ≥ 6 mg/mL (14.43 mM); Clear solution

      This protocol yields a clear solution of ≥ 6 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (60.0 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.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    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).
    Purity & Documentation

    Purity: 99.97%

    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, 1 year; -20°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 2.4053 mL 12.0267 mL 24.0535 mL 60.1337 mL
    5 mM 0.4811 mL 2.4053 mL 4.8107 mL 12.0267 mL
    10 mM 0.2405 mL 1.2027 mL 2.4053 mL 6.0134 mL
    15 mM 0.1604 mL 0.8018 mL 1.6036 mL 4.0089 mL
    20 mM 0.1203 mL 0.6013 mL 1.2027 mL 3.0067 mL
    25 mM 0.0962 mL 0.4811 mL 0.9621 mL 2.4053 mL
    30 mM 0.0802 mL 0.4009 mL 0.8018 mL 2.0045 mL
    40 mM 0.0601 mL 0.3007 mL 0.6013 mL 1.5033 mL
    50 mM 0.0481 mL 0.2405 mL 0.4811 mL 1.2027 mL
    60 mM 0.0401 mL 0.2004 mL 0.4009 mL 1.0022 mL
    80 mM 0.0301 mL 0.1503 mL 0.3007 mL 0.7517 mL
    100 mM 0.0241 mL 0.1203 mL 0.2405 mL 0.6013 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Clozapine N-oxide dihydrochloride Related Classifications

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    • 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.

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