| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C, protect from light, stored under nitrogen | [solubility ]
DMSO: 100 mg/mL (320.14 mM) | [form ]
Solid | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
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].
| 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.
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Store at -20°C, protect from light, stored under nitrogen | [References]
[1] Zhu X, et al. JHU-083 selectively blocks glutaminase activity in brain CD11b+ cells and prevents depression-associated behaviors induced by chronic social defeat stress. Neuropsychopharmacology. 2019 Mar;44(4):683-694. DOI:10.1038/s41386-018-0177-7
[2] Riggle BA, et al. MRI demonstrates glutamine antagonist-mediated reversal of cerebral malaria pathology in mice. Proc Natl Acad Sci U S A. 2018 Dec 18;115(51):E12024-E12033. DOI:10.1073/pnas.1812909115 |
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