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> JD-5037 [1392116-14-1]

JD-5037 [1392116-14-1]

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Cat# HY-18697-5mg

Size : 5mg

Marca : MedChemExpress

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

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JD-5037 Chemical Structure

JD-5037 Chemical Structure

CAS No. : 1392116-14-1

This product is a controlled substance and not for sale in your territory.

Based on 8 publication(s) in Google Scholar

    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.

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    Description

    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.
    Masse moléculaire

    572.51

    Formule

    C27H27Cl2N5O3S
    CAS No.

    1392116-14-1
    Unlabeled 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
    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 : 250 mg/mL (436.67 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 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.

    • 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: ≥ 2.75 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.
    Pureté et documentation

    Purity: 98.05%

    COA (262 KB) HNMR (191 KB) LCMS (347 KB)

    Instruction de manipulation (2659 KB)
    Références

    • [1]. Chorvat RJ. Peripherally restricted CB1 receptor blockers. Bioorg Med Chem Lett. 2013 Sep 1;23(17):4751-60.  [Content Brief]

      [2]. Knani I, et al. Targeting the endocannabinoid/CB1 receptor system for treating obesity in Prader-Willi syndrome. Mol Metab. 2016 Oct 22;5(12):1187-1199.  [Content Brief]

      [3]. Mukhopadhyay B, et al. Cannabinoid receptor 1 promotes hepatocellular carcinoma initiation and progression through multiple mechanisms. Hepatology. 2015 May;61(5):1615-26.  [Content Brief]

    Administration animale
    [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 n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.
    Références

    • [1]. Chorvat RJ. Peripherally restricted CB1 receptor blockers. Bioorg Med Chem Lett. 2013 Sep 1;23(17):4751-60.  [Content Brief]

      [2]. Knani I, et al. Targeting the endocannabinoid/CB1 receptor system for treating obesity in Prader-Willi syndrome. Mol Metab. 2016 Oct 22;5(12):1187-1199.  [Content Brief]

      [3]. Mukhopadhyay B, et al. Cannabinoid receptor 1 promotes hepatocellular carcinoma initiation and progression through multiple mechanisms. Hepatology. 2015 May;61(5):1615-26.  [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 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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    JD-5037 Related Classifications

    Help & FAQs

    Keywords:

    JD-50371392116-14-1JD5037JD 5037Cannabinoid ReceptorInhibitorinhibitorinhibit

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