1229591-56-3

1229591-56-3结构式

常用中文名：UCPH-102
常用英文名：UCPH-102
CAS号：1229591-56-3
分子式：C₂₁H₁₈N₂O₂
分子量：330.380
相关类别：研究领域癌症
发布时间：2018-06-11 18:56:28
更新时间：2024-07-18 19:22:23
UCPH-102是一种高选择性EAAT1抑制剂,IC50为0.43µM。UCPH-102对T-ALL细胞具有特异性抗增殖作用。UCPH-102还显示出良好的血脑通透性,可用于肌萎缩侧索硬化症、阿尔茨海默病、慢性疼痛和强迫症的研究[1][2][3][4]。

英文名	UCPH-102
英文别名	4H-1-Benzopyran-3-carbonitrile, 2-amino-5,6,7,8-tetrahydro-4-methyl-7-(1-naphthalenyl)-5-oxo- 2-Amino-4-methyl-7-(naphthalen-1-yl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile UCPH-102 2-Amino-4-methyl-7-(1-naphthyl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile 2-Amino-5,6,7,8-tetrahydro-4-methyl-7-(1-naphthalenyl)-5-oxo-4H-1-benzopyran-3-carbonitrile

描述	UCPH-102是一种高选择性EAAT1抑制剂,IC50为0.43µM。UCPH-102对T-ALL细胞具有特异性抗增殖作用。UCPH-102还显示出良好的血脑通透性,可用于肌萎缩侧索硬化症、阿尔茨海默病、慢性疼痛和强迫症的研究[1][2][3][4]。
相关类别	研究领域 >> 癌症信号通路 >> 其他 >> 其他研究领域 >> 神经疾病
靶点	IC50: 0.43 µM (EAAT1)[1].
参考文献	[1]. Huynh TH, et al. Design, synthesis and pharmacological characterization of coumarin-based fluorescent analogs of excitatory amino acid transporter subtype 1 selective inhibitors, UCPH-101 and UCPH-102. Bioorg Med Chem. 2012 Dec 1;20(23):6831-9. [2]. Haym I, et al. Bioavailability Studies and in vitro Profiling of the Selective Excitatory Amino Acid Transporter Subtype 1 (EAAT1) Inhibitor UCPH-102. ChemMedChem. 2016 Feb 17;11(4):403-19. [3]. Stanulović V S, et al. Proliferation and Survival of T-cell Acute Lymphoblastic Leukaemia Depends on mTOR-regulated Glutamine Uptake and EAAT1-dependent Conversion of Glutamine to Aspartate and Nucleotides. bioRxiv. 2020. [4]. Abrahamsen B, et al. Allosteric modulation of an excitatory amino acid transporter: the subtype-selective inhibitor UCPH-101 exerts sustained inhibition of EAAT1 through an intramonomeric site in the trimerization domain. J Neurosci. 2013 Jan 16;33(3):1068-87.