生物活性

Indoximod激活Trp充足信号而刺激mTOR，并解除IDO诱导的Trp缺乏和自体吞噬响应。Indoximod (D-1MT, NLG8189)以两种具有潜在不同生物学特性的立体异构体存在。L异构体是在纯化酶和基于HeLa细胞的测定中更有效的IDO活性抑制剂。而D异构体在逆转由表达IDO的树突细胞产生的T细胞的抑制方面显得更为有效。

体内研究中，口服联合给予dl-1-methyl-tryptophan与紫杉醇，可引起原发性乳腺肿瘤的消退。在移植的黑色素瘤和移植的原生乳腺癌小鼠模型中，Indoximod (400 mg/kg p.o.) 结合化学免疫疗法增强抗肿瘤免疫力。

To prepare 1MT for oral gavage, 1 g of 1MT was added to a 15 ml conical tube with 7.8 ml Methocel/Tween [0.5% Tween 80/0.5% Methylcellulose (v/v in water)]. The mixture was bead milled overnight by adding 1-2 ml by volume of 3 mm glass beads (Fisher) and mixing by inversion. The next day, the 1MT concentration was adjusted to 85 mg/ml by adding an additional 4 ml Methocel/Tween and mixing again briefly. The 1MT slurry was administered by oral gavage at 400 mg/kg/dose (0.1 cc/20 g mouse) using a curved feeding needle (20 G x 1 1/2 in; Fisher). For bid (twice a day) dosing, 1MT was administered once in the morning and once in the evening.

For administration in drinking water, D-1MT was prepared at 2 mg/ml in water as described above, supplemented with a small amount of aspartame (2 envelopes per liter) to improve acceptance by the mice, and filter sterilized. The solution was delivered in standard autoclaved drinking-water bottles. Mice drank 4.5-5.0 ml/day (similar to consumption of water without drug).

化学数据

实验操作 来自于公开的文献，仅供相同实验参考（如实验材料、目的不同，请参考其他文献）

不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的K_m系数（3），再除以大鼠的K_m系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。

储备液配制

以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。