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说明： Potent and selective EAAT1 and EAAT2 blocker
化学名： (3S)-3-[[3-[[4-(Trifluoromethyl)benzoyl]amino]phenyl]methoxy]-L-aspartic acid
纯度： ≥98% (HPLC)
生物活性 for TFB-TBOA
TFB-TBOA is a potent and selective glial glutamate transporter EAAT1 and EAAT2 inhibitor (IC50 values are 17, 22 and 300 nM for EAAT2, EAAT1 and EAAT3, respectively). Exhibits selectivity for EAAT1 and EAAT2 over EAAT4 and EAAT5, and a wide range of neuronal receptors and transporters. In HEK293 cells expressing human EAAT1, 2, and 3, TFB-TBOA exhibited selectivity for hEAAT1 and hEAAT2 over hEAAT3 (respective IC50 values are 3.6, 10, and 120 nM), while in tsA201 cells expressing rat EAAT4, [3H]-d-Asp uptake was inhibited with an IC50 of 40 nM. Attenuates glutamate-stimulated intracellular Na+ elevation in astrocytes in vitro (IC50 = 43 nM). Induces severe convulsions in vivo.
化合物库 for TFB-TBOA
TFB-TBOA is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for TFB-TBOA
| 分子量 | 426.35 |
| 公式 | C19H17F3N2O6 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 480439-73-4 |
| PubChem ID | 52941382 |
| InChI Key | LPWONNPEPDHEAI-GJZGRUSLSA-N |
| Smiles | OC([C@@H](N)[C@H](OCC1=CC=CC(NC(C2=CC=C(C(F)(F)F)C=C2)=O)=C1)C(O)=O)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for TFB-TBOA
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 21.32 | 50 |
制备储备液 for TFB-TBOA
以下数据基于产品分子量 426.35。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 4.69 mL | 23.45 mL | 46.91 mL |
| 2.5 mM | 0.94 mL | 4.69 mL | 9.38 mL |
| 5 mM | 0.47 mL | 2.35 mL | 4.69 mL |
| 25 mM | 0.09 mL | 0.47 mL | 0.94 mL |
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产品说明书 for TFB-TBOA
参考文献 for TFB-TBOA
参考文献是支持产品生物活性的出版物。
Tsukada et al (2005) Effects of a novel glutamate transporter blocker, (2S, 3S)-3-{3-[4-(trifluoromethyl)benzoylamino]benzyloxy}aspartate (TFB-TBOA), on activities of hippocampal neurons. Neuropharmacology 48 479 PMID: 15755476
Shimamoto and Shigeri (2006) Elucidation of glutamate transporter functions using selective inhibitors. CNS Agents Med.Chem. 6 59
Magi et al (2012) Physical and functional interaction of NCX1 and EAAC1 transporters leading to glutamate-enhanced ATP production in brain mitochondria. PLoS One 7 e34015 PMID: 22479505
Bozzo and Chatton (2010) Inhibitory effects of (2S, 3S)-3-[3-[4-(trifluoromethyl)benzoylamino]benzyloxy]aspartate (TFB-TBOA) on the astrocytic sodium responses to glutamate. Brain Res. 1316 PMID: 20026319
Fu et al (2018) Chemoenzymatic synthesis and pharmacological characterization of functionalized aspartate analogues as novel excitatory amino acid transporter inhibitors. J.Med.Chem. 61 7741 PMID: 30011368
If you know of a relevant reference for TFB-TBOA, please let us know.
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关键词: TFB-TBOA, TFB-TBOA supplier, High, affinity, EAAT1, EAAT2, blockers, EAAT, Excitatory, Amino, Acid, Transporters, GLAST, GLT-1, Glutamate, Monoamine, Neurotransmitter, 2532, Tocris Bioscience
13 篇 TFB-TBOA 的引用文献
引用文献是使用了 Tocris 产品的出版物。 TFB-TBOA 的部分引用包括：
Belozor et al (2019) Extracellular S100β Disrupts Bergman Glia Morphology and Synaptic Transmission in Cerebellar Purkinje Cells. Brain Sci 9 PMID: 31013844
Zhang et al (2019) Müller Glial Cells Participate in Retinal Waves via Glutamate Transporters and AMPA Receptors. Cell Rep 27 2871 PMID: 31167134
Martinez et al (2020) Loss of excitatory amino acid transporter restraint following chronic intermittent hypoxia contributes to synaptic alterations in nucleus tractus solitarii. J.Neurophysiol. 123 2122 PMID: 32347148
Obba et al (2015) The PRKAA1/AMPKα1 pathway triggers autophagy during CSF1-induced human monocyte differentiation and is a potential target in CMML. Mol Pain 11 1114 PMID: 26029847
Yan et al (2015) PacT. induces acute pain via directly activating toll like receptor 4. Physiol Rep 11 10 PMID: 25868824
Fleischer et al (2015) High-frequency voltage oscillations in cultured astrocytes. PLoS One 3 PMID: 25969464
O'Donnell et al (2016) Transient Oxygen/Glucose Deprivation Causes a Delayed Loss of Mitochondria and Increases Spontaneous Calcium Signaling in Astrocytic Processes. J Neurosci 36 7109 PMID: 27383588
Ivanov et al (2014) Glycolysis and oxidative phosphorylation in neurons and astrocytes during network activity in hippocampal slices. J Cereb Blood Flow Metab 34 397 PMID: 24326389
Chai et al (2017) Neural Circuit-Specialized Astrocytes: Transcriptomic, Proteomic, Morphological, and Functional Evidence. Neuron 95 531 PMID: 28712653
Zou et al (2011) Morphine potentiates neurodegenerative effects of HIV-1 Tat through actions at μ-opioid receptor-expressing glia. Brain 134 3616 PMID: 22102648
Rocchio et al (2019) Gene expression, proteome and calcium signaling alterations in immortalized hippocampal astrocytes from an Alzheimer's disease mouse model. Cell Death Dis 10 24 PMID: 30631041
Canul-Tec (2017) Structure and allosteric inhibition of excitatory amino acid transporter 1. Nature PMID: 28424515
Afzalov et al (2013) Low micromolar Ba(2+) potentiates glutamate transporter current in hippocampal astrocytes. Front Cell Neurosci 7 135 PMID: 24009556
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
Huntington's Disease Poster
Huntington's disease (HD) is a severe monogenic neurodegenerative disorder, which is characterized by the prevalent loss of GABAergic medium spiny neurons (MSN) in the striatum. This poster summarizes the effects of mutant huntingtin aggregation implicated in the pathology of HD, as well as highlighting the use of iPSCs for HD modeling.