1. GPCR/G Protein Neuronal Signaling
  2. Cannabinoid Receptor
  3. JD-5037

JD-5037 is a potent CB1R antagonist with an IC50 of 1.5 nM.

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No. CAS : 1392116-14-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
En stock
Solution
10 mM * 1 mL in DMSO En stock
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Revisión del cliente

Based on 9 publication(s) in Google Scholar

Other Forms of JD-5037:

Top Publications Citing Use of Products

    JD-5037 purchased from MedChemExpress. Usage Cited in: J Am Soc Nephrol. 2017 Dec;28(12):3518-3532.  [Abstract]

    The peripheral blockade of CB1R by JD5037 (3 mg/kg, administered orally) significantly normalizes the expression levels of pLKB1.

    Ver todos los productos específicos de isoformas Cannabinoid Receptor:

    • Actividad biológica

    • Protocolo

    • Pureza y Documentación

    • Referencias

    • Revisión del cliente

    Descripciòn

    JD-5037 is a potent CB1R antagonist with an IC50 of 1.5 nM.

    IC50 & Target

    CB1

    1.5 nM (IC50)

    In Vivo

    JD5037 (3 mg/kg/d, i.p.) induces equal reductions in body weight, attenuates the HFD-induced hyperglycemia, and reduces the HFD-induced hepatic injury and steatosis in obese Magel2-null mice[2].
    JD5037 (3 mg/kg/day, p.o.) significantly reduces the size of tumors and abrogates the tumor in DEN-treated mice. JD5037 attenuates the AEA levels in HCC samples from mice[3].

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

    Peso molecular

    572.51

    Fòrmula

    C27H27Cl2N5O3S

    No. CAS
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    NC([C@H](C(C)C)/N=C(NS(=O)(C1=CC=C(Cl)C=C1)=O)\N2N=C(C3=CC=C(Cl)C=C3)[C@@H](C4=CC=CC=C4)C2)=O

    Envío

    Room temperature in continental US; may vary elsewhere.

    Almacenamiento
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvente y solubilidad
    In Vitro: 

    DMSO : 100 mg/mL (174.67 mM; ultrasonic and warming and heat to 60°C; 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 1.7467 mL 8.7335 mL 17.4669 mL
    5 mM 0.3493 mL 1.7467 mL 3.4934 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.

    • 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: ≥ 2.75 mg/mL (4.80 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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: ≥ 2.75 mg/mL (4.80 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.75 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 (27.5 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: 99.38%

    Referencias
    Administraciòn de animales
    [2]

    Mice: JD-5037 is formulated in vehicle (V; 1% Tween80, 4% DMSO, 95% Saline). Obese mice are treated chronically (28 d) with vehicle (V; 1% Tween80, 4% DMSO, 95% Saline), JD5037, or SLV319 at a dose of 3 mg/kg, i.p. Body weight and food intake are monitored daily. Mice are euthanized by cervical dislocation under anesthesia; the brain, hypothalamus, liver, and combined fat pads are removed, weighed, and snap-frozen, and trunk blood is collected for determining the endocrine and biochemical parameters[2].

    MCE no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.

    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, 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 1.7467 mL 8.7335 mL 17.4669 mL 43.6674 mL
    5 mM 0.3493 mL 1.7467 mL 3.4934 mL 8.7335 mL
    10 mM 0.1747 mL 0.8733 mL 1.7467 mL 4.3667 mL
    15 mM 0.1164 mL 0.5822 mL 1.1645 mL 2.9112 mL
    20 mM 0.0873 mL 0.4367 mL 0.8733 mL 2.1834 mL
    25 mM 0.0699 mL 0.3493 mL 0.6987 mL 1.7467 mL
    30 mM 0.0582 mL 0.2911 mL 0.5822 mL 1.4556 mL
    40 mM 0.0437 mL 0.2183 mL 0.4367 mL 1.0917 mL
    50 mM 0.0349 mL 0.1747 mL 0.3493 mL 0.8733 mL
    60 mM 0.0291 mL 0.1456 mL 0.2911 mL 0.7278 mL
    80 mM 0.0218 mL 0.1092 mL 0.2183 mL 0.5458 mL
    100 mM 0.0175 mL 0.0873 mL 0.1747 mL 0.4367 mL
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    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.

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    Inquiry Information

    Nombre del producto:
    JD-5037
    Cat. No.:
    HY-18697
    Cantidad:
    MCE Japan Authorized Agent: