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.
性状
Solid
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[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.[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.
溶解度数据
In Vitro: Ethanol : 133.33 mg/mL (426.85 mM; Need ultrasonic)DMSO : 100 mg/mL (320.14 mM; Need ultrasonic)H2O : 50 mg/mL (160.07 mM; Need ultrasonic)