1. Metabolic Enzyme/Protease
  2. Glutaminase
  3. JHU-083

JHU-083, a proagent of 6-diazo-5-oxo-L-norleucine (DON; HY-108357), is an orally active and selective glutaminase antagonist. JHU-083 blocks glutaminase activity in brain CD11b+ cells and experimental cerebral malaria (ECM) resulting in a net decrease of glutamate levels in the animals.

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

JHU-083 Chemical Structure

JHU-083 Chemical Structure

CAS No. : 1998725-11-3

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1 mg USD 270 In-stock
5 mg USD 570 In-stock
10 mg USD 930 In-stock
50 mg   Get quote  
100 mg   Get quote  

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Customer Review

Based on 5 publication(s) in Google Scholar

Top Publications Citing Use of Products

    JHU-083 purchased from MedChemExpress. Usage Cited in: Front Immunol. 2022 May 19;13:880262.  [Abstract]

    JHU-083 (0.3mg/kg; i.v; single) significantly decreases TUNEL-positive cells in mice, which indicates that JHU-083 ameliorates the progression of ConA-induced autoimmune hepatitis by blocking glutamine metabolism in mice.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    JHU-083, a proagent of 6-diazo-5-oxo-L-norleucine (DON; HY-108357), is an orally active and selective glutaminase antagonist. JHU-083 blocks glutaminase activity in brain CD11b+ cells and experimental cerebral malaria (ECM) resulting in a net decrease of glutamate levels in the animals[1][2].

    In Vivo

    JHU-083 (1.82 mg/kg; PO; every other day for 12 days) ameliorates social avoidance behavior and anhedonia-like behavior induced by CSDS[1].
    JHU-083 (1.82 mg/kg, PO) attenuates CSDS-induced increase in glutaminase activity in CD11b+ cells in the prefrontal cortex and hippocampus, but not in the cerebellum. JHU-083 treatment suppresses the CSDS-induced upregulation of IL-1β and TNF-α expression[1].

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

    Animal Model: Male 7-to 8-week-old C57BL/6J (C57) mice (25-30 g) with chronic social defeat stress (CSDS)[1]
    Dosage: 1.82 mg/kg
    Administration: PO; every other day for 12 days
    Result: Ameliorated social avoidance behavior and anhedonia-like behavior induced by CSDS.
    Molecular Weight

    312.36

    Formula

    C14H24N4O4

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C(OCC)[C@H](CCC(C=[N+]=[N-])=O)NC([C@H](CC(C)C)N)=O

    Shipping

    Shipping with dry ice.

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    Solvent & Solubility
    In Vitro: 

    Ethanol : 133.33 mg/mL (426.85 mM; Need ultrasonic)

    DMSO : 100 mg/mL (320.14 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 50 mg/mL (160.07 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.2014 mL 16.0072 mL 32.0143 mL
    5 mM 0.6403 mL 3.2014 mL 6.4029 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

    * 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

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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: ≥ 2.5 mg/mL (8.00 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 (8.00 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:

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    Dosing volume
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    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: ≥98.0%

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO / Ethanol 1 mM 3.2014 mL 16.0072 mL 32.0143 mL 80.0359 mL
    5 mM 0.6403 mL 3.2014 mL 6.4029 mL 16.0072 mL
    10 mM 0.3201 mL 1.6007 mL 3.2014 mL 8.0036 mL
    15 mM 0.2134 mL 1.0671 mL 2.1343 mL 5.3357 mL
    20 mM 0.1601 mL 0.8004 mL 1.6007 mL 4.0018 mL
    25 mM 0.1281 mL 0.6403 mL 1.2806 mL 3.2014 mL
    30 mM 0.1067 mL 0.5336 mL 1.0671 mL 2.6679 mL
    40 mM 0.0800 mL 0.4002 mL 0.8004 mL 2.0009 mL
    50 mM 0.0640 mL 0.3201 mL 0.6403 mL 1.6007 mL
    60 mM 0.0534 mL 0.2668 mL 0.5336 mL 1.3339 mL
    80 mM 0.0400 mL 0.2001 mL 0.4002 mL 1.0004 mL
    100 mM 0.0320 mL 0.1601 mL 0.3201 mL 0.8004 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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    JHU-083 Related Classifications

    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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    Product Name:
    JHU-083
    Cat. No.:
    HY-122218
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