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.
Product information
CAS Number: 1998725-11-3
Molecular Weight: 312.36
Formula: C14H24N4O4
Chemical Name: ethyl (2S)-2-[(2S)-2-amino-4-methylpentanamido]-6-diazo-5-oxohexanoate
Smiles: CC(C)C[C@H](N)C(=O)N[C@@H](CCC(=O)C=[N+]=[N-])C(=O)OCC
InChiKey: YZRCHOFKIPHQBW-RYUDHWBXSA-N
InChi: InChI=1S/C14H24N4O4/c1-4-22-14(21)12(6-5-10(19)8-17-16)18-13(20)11(15)7-9(2)3/h8-9,11-12H,4-7,15H2,1-3H3,(H,18,20)/t11-,12-/m0/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 100 mg/mL (320.14 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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. 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.
Products are for research use only. Not for human use.
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