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

JHU-083 

Cat. No.: HY-122218 Purity: >97.0%
Handling Instructions

JHU-083, a prodrug 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

Size Price Stock Quantity
1 mg USD 320 In-stock
Estimated Time of Arrival: December 31
5 mg USD 650 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

JHU-083, a prodrug 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].

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.

1998725-11-3

SMILES

O=C(OCC)[[email protected]](CCC(C=[N+]=[N-])=O)NC([[email protected]](CC(C)C)N)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light, stored under nitrogen

*The compound is unstable in solutions, freshly prepared is recommended.

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (320.14 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
10 mM 0.3201 mL 1.6007 mL 3.2014 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (8.00 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: >97.0%

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Keywords:

JHU-083JHU083JHU 083Glutaminase6-diazo-5-oxo-L-norleucineDONorallybrainCD11b+experimentalcerebralmalariaECMInhibitorinhibitorinhibit

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Product name:
JHU-083
Cat. No.:
HY-122218
Quantity:
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