Powder: -20°C for 3 years | In solvent: -80°C for 1 year
680C91 是一种具有口服活性的色氨酸 2,3-双加氧酶 (TDO) 选择性抑制剂(Ki:51 nM)。它可用于研究肿瘤免疫及阿尔茨海默症。其中TDO 是色氨酸分解代谢的关键酶。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 282 | 现货 | ||
2 mg | ¥ 385 | 现货 | ||
5 mg | ¥ 538 | 现货 | ||
10 mg | ¥ 872 | 现货 | ||
25 mg | ¥ 1,680 | 现货 | ||
50 mg | ¥ 2,730 | 现货 | ||
100 mg | ¥ 3,920 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 822 | 现货 |
产品描述 | 680C91 is a potent and selective inhibitor of TDO, and its Ki is 51 nM. |
靶点活性 | TDO:51 nM(Ki) |
体外活性 | 68OC91, a potent (Ki = 51 nM) and selective TDO inhibitor, has no inhibitory activity against monoamine oxidase A and B, indoleamine 2,3-dioxygenase (EC 1.13.11.17), 5-HT uptake and 5-HT1A,5-HT1D,5-HT2A and 5-HT2c receptors at a concentration of 10 μM. 68OC91 has no effect on the binding of tryptophan to albumin in plasma and inhibited TDO competitively with respect to its substrate tryptophan. 68OC91 inhibits the catabolism of tryptophan by rat liver cells and rat liver perfused in situ.[1] |
体内活性 | Prior administration of 68OC91 inhibits the catabolism of L-[ring-2-14C]-tryptophan and a load dose of tryptophan (100 mg/kg) in vivo. Administration of 68OC91 alone significantly increases brain tryptophan, 5-HIAA and 5-HT. A load dose of tryptophan (100 mg/kg), producing increases in brain tryptophan 4-fold greater than that seen with 68OC91, does not increase brain 5-HIAA and 5-HT to levels greater than those seen with 68OC91 and produces a shorter-lasting increase in these parameters.[1] |
细胞实验 | Cell lines: rat liver cells. Concentrations: 0.1 μM, 0.5 μM, 2 μM. Incubation Time: 0 min - 120 min. Method: The combined concentration of non-labelled L-tryptophan and the L-[ring-2-14C]-tryptophan used in the assays is 20 μM and is added either with or without 68OC91 at time zero. |
动物实验 | Animal Models: Male Wistar rats. Dosages: 15 mg/kg. Administration: Oral gavage |
分子量 | 238.26 |
分子式 | C15H11FN2 |
CAS No. | 163239-22-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (209.85 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 4.1971 mL | 20.9855 mL | 41.971 mL | 104.9274 mL |
5 mM | 0.8394 mL | 4.1971 mL | 8.3942 mL | 20.9855 mL | |
10 mM | 0.4197 mL | 2.0985 mL | 4.1971 mL | 10.4927 mL | |
20 mM | 0.2099 mL | 1.0493 mL | 2.0985 mL | 5.2464 mL | |
50 mM | 0.0839 mL | 0.4197 mL | 0.8394 mL | 2.0985 mL | |
100 mM | 0.042 mL | 0.2099 mL | 0.4197 mL | 1.0493 mL |
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。
680C91 163239-22-3 Others inhibit Inhibitor tryptophan 2,3-dioxygenasetryptophan catabolismAlzheimer’s Disease 680C-91 inhibitor