UCPH-102

• 常用名: UCPH-102
• 英文名: UCPH-102
• CAS号: 1229591-56-3
• 分子量: 330.380
• 密度: 1.3±0.1 g/cm3
• 沸点: 610.7±55.0 °C at 760 mmHg
• 分子式: C₂₁H₁₈N₂O₂
• 熔点: N/A
• 闪点: 323.2±31.5 °C

UCPH-102用途

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]。

UCPH-102名称

• 英文名: UCPH-102

UCPH-102生物活性

• 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.

UCPH-102物理化学性质

• 密度: 1.3±0.1 g/cm3
• 沸点: 610.7±55.0 °C at 760 mmHg
• 分子式: C₂₁H₁₈N₂O₂
• 分子量: 330.380
• 闪点: 323.2±31.5 °C
• 精确质量: 330.136841
• LogP: 2.68
• 蒸汽压: 0.0±1.8 mmHg at 25°C
• 折射率: 1.676

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