TFB-TBOA

• 常用名: TFB-TBOA
• 英文名: TFB-TBOA
• CAS号: 480439-73-4
• 分子量: 426.34300
• 密度: N/A
• 沸点: N/A
• 分子式: C₁₉H₁₇F₃N₂O₆
• 熔点: N/A
• 闪点: N/A

TFB-TBOA用途

TFB-TBOA(CF3-Bza-TBOA)是一种有效的谷氨酸转运体阻滞剂,可有效抑制神经胶质转运体的活性。TFB-TBOA显示,在使用瞬时表达EAATs的细胞进行的摄取试验中,谷氨酸转运体EAAT1、EAAT2和EAAT3的IC50值分别为22、17和300 nM[1]。

TFB-TBOA名称

• 英文名: TFB-TBOA,(3S)-3-[[3-[[4-(Trifluoromethyl)benzoyl]amino]phenyl]methoxy]-L-asparticacid

TFB-TBOA生物活性

• 描述: TFB-TBOA(CF3-Bza-TBOA)是一种有效的谷氨酸转运体阻滞剂,可有效抑制神经胶质转运体的活性。TFB-TBOA显示,在使用瞬时表达EAATs的细胞进行的摄取试验中,谷氨酸转运体EAAT1、EAAT2和EAAT3的IC50值分别为22、17和300 nM[1]。
• 相关类别:
  信号通路 >> 跨膜转运 >> EAAT2
  研究领域 >> 神经疾病
• 体外研究: TFB-TBOA(CF3-Bza-TBOA)以剂量依赖性的方式抑制大鼠海马脑片辐射层星形胶质细胞中的突触激活转运体电流(STC),IC50为13 nM,并在100 nM时将其降低至对照的约10%[2]。TFB-TBOA以浓度依赖性方式抑制200µM谷氨酸诱发的钠+碘反应,IC50值为43 nM,根据钠+碘反应的振幅测量[1]。
• 参考文献:

  [1]. Shimamoto K, et al. Characterization of novel L-threo-beta-benzyloxyaspartate derivatives, potent blockers of the glutamate transporters. Mol Pharmacol. 2004;65(4):1008-1015.

  [2]. Tsukada S, et al. Effects of a novel glutamate transporter blocker, (2S, 3S)-3-[3-[4-(trifluoromethyl)benzoylamino]benzyloxy]aspartate (TFB-TBOA), on activities of hippocampal neurons. Neuropharmacology. 2005;48(4):479-491.

  [3]. Bozzo L, et al. Inhibitory effects of (2S, 3S)-3-[3-[4-(trifluoromethyl)benzoylamino]benzyloxy]aspartate (TFB-TBOA) on the astrocytic sodium responses to glutamate. Brain Res. 2010;1316:27-34.

TFB-TBOA物理化学性质

• 分子式: C₁₉H₁₇F₃N₂O₆
• 分子量: 426.34300
• 精确质量: 426.10400
• PSA: 138.95000
• LogP: 3.11270
• InChIKey: LPWONNPEPDHEAI-GJZGRUSLSA-N
• SMILES: NC(C(=O)O)C(OCc1cccc(NC(=O)c2ccc(C(F)(F)F)cc2)c1)C(=O)O

TFB-TBOA靶点实验

查看更多实验

实验名称：Inhibition of human EAAT1 expressed in HEK293 cells assessed as reduction in [3H]-D-A... 来源：ChEMBL 靶标：Excitatory amino acid transporter 1 External Id：CHEMBL4150966

实验名称：Inhibition of human EAAT2 expressed in HEK293 cells assessed as reduction in [3H]-D-A... 来源：ChEMBL 靶标：Excitatory amino acid transporter 2 External Id：CHEMBL4150967

实验名称：Inhibition of human EAAT3 expressed in HEK293 cells assessed as reduction in [3H]-D-A... 来源：ChEMBL 靶标：Excitatory amino acid transporter 3 External Id：CHEMBL4150968

实验名称：Inhibition of human GLT1 expressed in Xenopus laevis Oocytes assessed as reduction of... 来源：ChEMBL 靶标：Excitatory amino acid transporter 2 External Id：CHEMBL1259930

实验名称：Inhibition of human EAAC1 expressed in Xenopus laevis Oocytes assessed as reduction o... 来源：ChEMBL 靶标：Excitatory amino acid transporter 3 External Id：CHEMBL1259929

实验名称：Selectivity index, ratio of IC50 for human EAAT3 transfected in African green monkey ... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5382765

实验名称：Inhibition of rat EAAT4 expressed in tsA201 cells assessed as reduction in [3H]-D-Asp... 来源：ChEMBL 靶标：Excitatory amino acid transporter 4 External Id：CHEMBL4150969

实验名称：Selectivity index, ratio of IC50 for human EAAT1 transfected in African green monkey ... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5382761

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TFB-TBOA英文别名

• tfb-tboa