1. GPCR/G Protein Neuronal Signaling
  2. mAChR
  3. Deschloroclozapine

Deschloroclozapine, a metabolite of Clozapine, is a highly potent muscarinic DREADDs agonist, with blood-brain barrier permeability. Deschloroclozapine binds to DREADD receptor subtypes hM3Dq and hM4Di with Ki of 6.3 and 4.2 nM, respectively. [11C]-Deschloroclozapine is developed as a promising PET tracer for DREADD imaging.

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No. CAS : 1977-07-7

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10 mM * 1 mL in DMSO
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Revisión del cliente

Based on 83 publication(s) in Google Scholar

Other Forms of Deschloroclozapine:

Top Publications Citing Use of Products

83 Publications Citing Use of MCE Deschloroclozapine

IF
In Vivo Efficacy Study

    Deschloroclozapine purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Apr;12(13):e2406192.  [Abstract]

    Deschloroclozapine dihydrochloride (DCZ; 0.1 mg/kg; ip) showed mCh + DCZ‐, Gi + saline‐ and Gi + DCZ‐treated mice displayed normal sociability.

    Deschloroclozapine purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Apr;12(13):e2406192.  [Abstract]

    Deschloroclozapine dihydrochloride (DCZ; 0.1 mg/kg; ip) showed mCh + DCZ‐ and Gi + saline ‐treated mice displayed a marked preference for novel conspecifics, Gi + DCZ‐treated mice did not differentiate between familiar and novel mice.

    Deschloroclozapine purchased from MedChemExpress. Usage Cited in: Research (Wash D C). 2025 May 14:8:0701.  [Abstract]

    Representative immunofluorescent images of c-Fos (Green) in mCherry-positive MPOA GABAergic neurons (red) after saline or Deschloroclozapine (DCZ) (100 μg/kg; i.p.) treatment in GAD2-IRES-Cre mice.

    Deschloroclozapine purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Nov 2:2025.04.18.649578.

    Deschloroclozapine dihydrochloride (DCZ; 0.02 mg/kg; ip) caused an increase in SST interneuron responses in mice.

    Deschloroclozapine purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Nov 2:2025.04.18.649578.

    Deschloroclozapine dihydrochloride (DCZ; 0.02 mg/kg; ip) reduced activity in VIP interneurons and prevented S1 potentiation upon RWS stimulation alone. In the presence of DCZ, RWS stimulation suppresses L2/3 pyramidal cell potentiation, and even causes depression, even when the CF is not co-activated.

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    • Actividad biológica

    • Pureza y Documentación

    • Referencias

    • Revisión del cliente

    Descripciòn

    Deschloroclozapine, a metabolite of Clozapine, is a highly potent muscarinic DREADDs agonist, with blood-brain barrier permeability. Deschloroclozapine binds to DREADD receptor subtypes hM3Dq and hM4Di with Ki of 6.3 and 4.2 nM, respectively. [11C]-Deschloroclozapine is developed as a promising PET tracer for DREADD imaging[1][2][3].

    IC50 & Target

    mAChR3

     

    mAChR4

     

    In Vitro

    Designer Receptors Exclusively Activated by Designer Drugs (DREADD) are a chemogenetic approach for remote manipulation of neuronal activity in freely-moving animals. DREADDs comprise mutated G protein-coupled receptors (GPCRs) that do not respond to their endogenous neurotransmitter, but do respond to an otherwise “inert” exogenous substance[2].

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

    In Vivo

    Deschloroclozapine (0.3 mg/kg; intramuscularly) impairs working memory function in male rhesus macaques (aged between 5 and 6 years and weighing 5.5-7.9 kg)[3].
    Deschloroclozapine (0.1 mg/kg; i.m) is effective at activating DREADD receptors in vivo and reversibly inducing behavioral effects in monkeys[3].

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

    Peso molecular

    292.39

    Fòrmula

    C18H20N4

    No. CAS
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    CN1CCN(C2=NC3=CC=CC=C3NC4=CC=CC=C42)CC1

    Envío

    Room temperature in continental US; may vary elsewhere.

    Almacenamiento
    Powder -20°C 3 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvente y solubilidad
    In Vitro: 

    DMSO : 100 mg/mL (342.01 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 3.4201 mL 17.1004 mL 34.2009 mL
    5 mM 0.6840 mL 3.4201 mL 6.8402 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Calculadora de molaridad

    • Calculadora de dilución

    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 (8.55 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% Corn Oil

      Solubility: ≥ 2.5 mg/mL (8.55 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 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 (25.0 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)

    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.
    Pureza y Documentación

    Purity: 99.93%

    Referencias

    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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.4201 mL 17.1004 mL 34.2009 mL 85.5022 mL
    5 mM 0.6840 mL 3.4201 mL 6.8402 mL 17.1004 mL
    10 mM 0.3420 mL 1.7100 mL 3.4201 mL 8.5502 mL
    15 mM 0.2280 mL 1.1400 mL 2.2801 mL 5.7001 mL
    20 mM 0.1710 mL 0.8550 mL 1.7100 mL 4.2751 mL
    25 mM 0.1368 mL 0.6840 mL 1.3680 mL 3.4201 mL
    30 mM 0.1140 mL 0.5700 mL 1.1400 mL 2.8501 mL
    40 mM 0.0855 mL 0.4275 mL 0.8550 mL 2.1376 mL
    50 mM 0.0684 mL 0.3420 mL 0.6840 mL 1.7100 mL
    60 mM 0.0570 mL 0.2850 mL 0.5700 mL 1.4250 mL
    80 mM 0.0428 mL 0.2138 mL 0.4275 mL 1.0688 mL
    100 mM 0.0342 mL 0.1710 mL 0.3420 mL 0.8550 mL
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    Inquiry Information

    Nombre del producto:
    Deschloroclozapine
    Cat. No.:
    HY-42110
    Cantidad:
    MCE Japan Authorized Agent: