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GNF-PF-3777(8-Nitrotryptanthrin)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GNF-PF-3777(8-Nitrotryptanthrin)图片
CAS NO:77603-42-0
规格:98%
分子量:293.23
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
8-Nitrotryptanthrin是一种有效的人吲哚胺2,3-双加氧酶2(hIDO2)抑制剂,有效降低IDO2活性,Ki值为0.97μM。
CAS:77603-42-0
分子式:C15H7N3O4
分子量:293.23
纯度:98%
存储:Store at -20°C

Background:

8-Nitrotryptanthrin is a potent human indoleamine 2,3-dioxygenase 2 (hIDO2) inhibitor which significantly reduces IDO2 activity with Ki of 0.97 μM.


The typtanthrin derivative 8-Nitrotryptanthrin (5i) is found to be a potent hIDO2 inhibitor with superior efficiency far better than that of the most frequently-used inhibitor L-1-MT. The IC50 values show that all nine tryptanthrin compounds display hIDO2 inhibitory activities, especially, the compound 8-Nitrotryptanthrin demonstrates much stronger inhibition (1.87 μM) than both L-1-MT (82.53 μM) and D-1-MT (262.75 μM). 8-Nitrotryptanthrin exhibits significant antitrypanosomal activity with EC50 of 0.82 μM[2]. 8-Nitrotryptanthrin has a microplate Alamar Blue assay (MABA) minimum inhibitory concentration (MIC) value of 0.032 μg/mL. 8-Nitrotryptanthrin also has a LORA MIC value of 2.4 μg/mL, while the majority of analogues lack LORA activity[3].



[1]. Li J, et al. Establishment of a human indoleamine 2, 3-dioxygenase 2 (hIDO2) bioassay system and discovery of tryptanthrin derivatives as potent hIDO2 inhibitors. Eur J Med Chem. 2016 Nov 10;123:171-9. [2]. Scovill J, et al. Antitrypanosomal activities of tryptanthrins. Antimicrob Agents Chemother. 2002 Mar;46(3):882-3. [3]. Hwang JM, et al. Design, synthesis, and structure-activity relationship studies of tryptanthrins as antitubercular agents. J Nat Prod. 2013 Mar 22;76(3):354-67.