JHU-083
目录号: PL02530 纯度: ≥98%
CAS No. :1998725-11-3
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中文名称
JHU-083
英文名称
JHU-083
英文别名
Ethyl (2R)-2-[[(2R)-2-amino-4-methylpentanoyl]amino]-6-diazo-5-oxohexanoate;JHU-083
Cas No.
1998725-11-3
分子式
C14H24N4O4
分子量
312.36
包装储存
Please store the product under the recommended conditions in the Certificate of Analysis.
产品详情
JHU-083 是 6-diazo-5-oxo-L-norleucine (DON; HY-108357) 的前药,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。
生物活性
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)
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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