Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Indoximod (Indoximod (NLG-8189)) 是一种具有口服具有活力的吲哚胺2,3-双加氧酶(IDO) 途径抑制剂。它在调节 mTOR 中充当 Trp 模拟物。它是一种可用于癌症研究的免疫代谢佐剂。
产品描述 | Indoximod (Indoximod (NLG-8189)) is a methylated tryptophan with immune checkpoint inhibitory activity. Indoximod inhibits the enzyme indoleamine 2, 3-dioxygenase (IDO), which degrades the essential amino acid tryptophan, and may increase or maintain tryptophan levels important to T cell function. Tryptophan depletion is associated with immunosuppression involving T cell arrest and anergy. |
靶点活性 | IDO:19 μM(Ki) |
体外活性 | Indoximod significantly reverses the suppression of T cells created by IDO-expressing dendritic cells, using both human monocyte-derived dendritic cells and murine dendritic cells isolated directly from tumor-draining lymph nodes. [1] Indoximod activates a Trp sufficiency signal that stimulates mTOR, and relieves IDO-induced Trp deprivation as well as an autophagic response. [2] |
体内活性 | In mouse models of transplantable melanoma and transplantable and autochthonous breast cancer, Indoximod (400 mg/kg p.o.) enhances antitumor immunity in the setting of combined chemo-immunotherapy regimens. [1] |
激酶实验 | 1MT enantiomers are solubilized in DMSO containing 0.1N HCl and added at concentrations of 100, 50, and 0 μM to wells containing the reaction mixture with tryptophan (0-200 μM) followed by addition of IDO enzyme. Plates are sealed and incubated 1 hr in a humidified 37°C incubator, after which the reactions are terminated by addition of 12.5 μl 30% TCA per well. Plates are then resealed in plastic wrap, incubated 30 min at 50°C to hydrolyze the reaction product N-formylkynurenine to kynurenine, and centrifuged. Supernatants are transferred to a flat-bottom 96-well plate, mixed with 100 μl Ehrlich reagent and incubated 10 min at room temperature. Absorbance at 490 nm is read[1]. |
别名 | NLG-8189, Indoximod (NLG-8189), 1-Methyl-D-tryptophan, 吲哚莫德 |
分子量 | 218.25 |
分子式 | C12H14N2O2 |
CAS No. | 110117-83-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: Slightly soluble
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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