生物活性 | |||
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描述 | The typtanthrin derivative known as GNF-PF-3777, or 8-Nitrotryptanthrin, is a highly effective inhibitor of hIDO2, surpassing the commonly used L-1-MT in efficiency. The IC50 values indicate that all nine tryptanthrin derivatives inhibit hIDO2, with GNF-PF-3777 showing significantly stronger inhibition at 1.87 μM, compared to L-1-MT at 82.53 μM and D-1-MT at 262.75 μM. Additionally, GNF-PF-3777 has notable antitrypanosomal activity, with an EC50 of 0.82 μM[1]. In the microplate Alamar Blue assay, GNF-PF-3777's minimum inhibitory concentration (MIC) is 0.032 μg/mL, and it also has a LORA MIC of 2.4 μg/mL, whereas most analogues do not exhibit LORA activity[2]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.41mL 0.68mL 0.34mL |
17.05mL 3.41mL 1.71mL |
34.10mL 6.82mL 3.41mL |
参考文献 |
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