Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DL-TBOA ammonium is a potent, non-transportable inhibitor of excitatory amino acid transporters. Its inhibitory effects are demonstrated by IC50 values of 70 μM, 6 μM, and 6 μM for excitatory amino acid transporter-1 (EAAT1), EAAT2, and EAAT3, respectively. Additionally, DL-TBOA ammonium significantly hampers the uptake of [14C]glutamate in COS-1 cell lines expressing human EAAT1 and EAAT2, evident by Ki values of 42 μM and 5.7 μM, respectively. Furthermore, this compound competitively blocks EAAT4 and EAAT5, with Ki values of 4.4 μM and 3.2 μM, respectively.
产品描述 | DL-TBOA ammonium is a potent, non-transportable inhibitor of excitatory amino acid transporters. Its inhibitory effects are demonstrated by IC50 values of 70 μM, 6 μM, and 6 μM for excitatory amino acid transporter-1 (EAAT1), EAAT2, and EAAT3, respectively. Additionally, DL-TBOA ammonium significantly hampers the uptake of [14C]glutamate in COS-1 cell lines expressing human EAAT1 and EAAT2, evident by Ki values of 42 μM and 5.7 μM, respectively. Furthermore, this compound competitively blocks EAAT4 and EAAT5, with Ki values of 4.4 μM and 3.2 μM, respectively. |
靶点活性 | EAAT2 (human):5.7 μM (IC50), EAAT1 (human):Ki: 42 μM, EAAT4:4.4 μM (IC50), EAAT1:70 μM (IC50), EAAT5:3.2 μM (IC50), EAAT3:6 μM (IC50), EAAT2:6 μM (IC50) |
体外活性 | DL-TBOA ammonium (70-350 μM; 48 hours) treatment concentration-dependently enhances SN38-induced loss of viability. DL-TBOA reversed Oxaliplatin-induced loss of viability[4]. DL-TBOA ammonium (350 μM; 24 hours) decreases p53 induction by SN38 and oxaliplatin[4]. Cell Viability Assay[4]Cell Line: HCT116 cells, LoVo cells Concentration: 70 μM, 350 μM Incubation Time: 48 hours Result: Enhanced SN38-induced, and counteracted Oxaliplatin-induced, cell death. Cell Viability Assay[4]Cell Line: HCT116 cells, LoVo cells Concentration: 350 μM Incubation Time: 24 hours Result: Decreased p53 induction by SN38 and oxaliplatin. |
体内活性 | DL-TBOA ammonium (10 nmol; i.c.v.) to morphine-dependent rats significantly facilitates the expression of naloxone-precipitated somatic signs and conditioned place aversion[5]. Animal Model: Male Sprague-Dawley rats (180-250 g)[5]Dosage: 1 nmol, 3 nmol, 10 nmol Administration: Intracerebroventricularly injection (i.c.v.) Result: Dose dependently facilitated various somatic signs induced by Naloxone (0.1 mg/kg)-precipitated morphine withdrawal. |
分子量 | 256.258 |
分子式 | C11H16N2O5 |
CAS No. | 2093503-71-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
DL-TBOA ammonium 2093503-71-8 DLTBOA ammonium DL TBOA ammonium Inhibitor inhibitor inhibit