JHU-083

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

JHU-083 是 6-diazo-5-oxo-L-norleucine (DON) 的前体，是一种口服有效的，选择性的谷氨酰胺酶 (glutaminase) 拮抗剂，可阻断脑 CD11b+ 细胞和实验性脑疟疾 (ECM) 中的谷氨酰胺酶，导致动物中谷氨酸水平的净降低。

JHU-083, a proagent of 6-diazo-5-oxo-L-norleucine (DON), 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.

JHU-083 (1.82 mg/kg；口服；每隔一天一次，持续 12 天) 改善由 CSDS 诱导的社交回避行为和快感缺乏样行为。 JHU-083 (1.82 mg/kg；口服) 减弱 CSDS 诱导的前额皮质和海马 CD11b+ 细胞中谷氨酰胺酶活性的增加，但不影响小脑。JHU-083 处理可抑制 CSDS 诱导的 IL-1β 和 TNF-α 表达上调。Animal Model:Male 7-to 8-week-old C57BL/6J (C57) mice (25-30?g) with chronic social defeat stress (CSDS)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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Others

Other Targets

Glutamine

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1998725-11-3

312.37

C14H24N4O4

>98% (HPLC)

Ethanol : 133.33 mg/mL (426.85 mM; ultraphonic) DMSO : 100 mg/mL (320.14 mM; ultraphonic; ) H2O : 50 mg/mL (160.07 mM; ultraphonic)

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

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

(-20℃)

With Ice Pack

≥ 2 years