4-氧代-1,4-二氢-1,10-菲咯啉-3-羧酸

• 常用名: 4-氧代-1,4-二氢-1,10-菲咯啉-3-羧酸
• 英文名: 1,4-DPCA
• CAS号: 331830-20-7
• 分子量: 240.214
• 密度: 1.5±0.1 g/cm3
• 沸点: 474.5±45.0 °C at 760 mmHg
• 分子式: C₁₃H₈N₂O₃
• 熔点: N/A
• 闪点: 240.8±28.7 °C

4-氧代-1,4-二氢-1,10-菲咯啉-3-羧酸用途

1,4-DPCA,一种有效的选择性脯氨酰-4-羟化酶 (prolyl-4-hydroxylase) 抑制剂,也是人包皮成纤维细胞中的胶原蛋白羟基化抑制剂,IC50 为 2.4 µM。1,4-DPCA 抑制脯氨酰-4-羟化酶 α 同工型,可稳定 HIF-1α 蛋白。1,4-DPCA 还抑制 FIH,IC50 为 60 μM。

4-氧代-1,4-二氢-1,10-菲咯啉-3-羧酸名称

• 中文名: 4-氧代-1,4-二氢-1,10-菲咯啉-3-羧酸
• 英文名: 4-oxo-1,4-dihydro-[1,10]phenanthroline-3-carboxylic acid

4-氧代-1,4-二氢-1,10-菲咯啉-3-羧酸生物活性

• 描述: 1,4-DPCA,一种有效的选择性脯氨酰-4-羟化酶 (prolyl-4-hydroxylase) 抑制剂,也是人包皮成纤维细胞中的胶原蛋白羟基化抑制剂,IC50 为 2.4 µM。1,4-DPCA 抑制脯氨酰-4-羟化酶 α 同工型,可稳定 HIF-1α 蛋白。1,4-DPCA 还抑制 FIH,IC50 为 60 μM。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> 代谢酶/蛋白酶 >> HIF/HIF脯氨酰-羟化酶
• 靶点实验:

  IC50: 2.4 µM (Collagen hydroxylation); 60 μM (Factor inhibiting HIF (FIH))[2]

• 体外研究: 1,4-DPCA(24小时)治疗特别增加多个靶基因的表达,包括促血管生成的靶基因Vegfa和Hmox1以及促糖解靶点Ldh-a、Pgk1、Pdk1和Glut1在小鼠B6细胞中的表达[1]。1,4-DPCA处理显著降低T4-2(10μm1,4-DPCA)和ZR-75-1细胞(20μm1,4-DPCA)的菌落大小。1,4-DPCA处理的T4-2细胞在3D培养中形成极化球体。1,4-DPCA可显著降低DA-MB-157(20μM 1,4-DPCA)和MDA-MB-231(10μM 1,4-DPCA)细胞的侵袭性分支,1,4-DPCA可抑制T4-2、ZR-75-1、MDA-MB-157和MDA-MB-231细胞的增殖[3]。
• 体内研究: 1,4-DPCA治疗抑制小鼠腹腔植入多孔多孔聚乳酸-乙醇酸(PLGA)椎间盘结缔组织的生长。1,4-DPCA可有效抑制椎间盘内外的胶原沉积,也可限制结缔组织的生长,但对糖皮质激素的抑制作用不明显[2]。
• 参考文献:

  [1]. Yong Zhang, et al. Drug-induced regeneration in adult mice. Sci Transl Med. 2015 Jun 3;7(290):290ra92.

  [2]. Ryan J Love, et al. Transient inhibition of connective tissue infiltration and collagen deposition into porous poly(lactic-co-glycolic acid) discs. J Biomed Mater Res A. 2013 Dec;101(12):3599-606.

  [3]. Gaofeng Xiong, et al. Prolyl-4-hydroxylase α subunit 2 promotes breast cancer progression and metastasis by regulating collagen deposition. BMC Cancer. 2014 Jan 2;14:1.

4-氧代-1,4-二氢-1,10-菲咯啉-3-羧酸物理化学性质

• 密度: 1.5±0.1 g/cm3
• 沸点: 474.5±45.0 °C at 760 mmHg
• 分子式: C₁₃H₈N₂O₃
• 分子量: 240.214
• 闪点: 240.8±28.7 °C
• 精确质量: 240.053497
• PSA: 83.05000
• LogP: 3.28
• 蒸汽压: 0.0±1.2 mmHg at 25°C
• 折射率: 1.727

4-氧代-1,4-二氢-1,10-菲咯啉-3-羧酸安全信息

• 海关编码: 2933990090

4-氧代-1,4-二氢-1,10-菲咯啉-3-羧酸海关

• 海关编码: 2933990090
• 中文概述: 2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%
• 申报要素: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期
• Summary: 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

4-氧代-1,4-二氢-1,10-菲咯啉-3-羧酸靶点实验

查看更多实验

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实验名称：Antitubercular activity against Mycobacterium tuberculosis H37Rv measured after 7 day... 来源：ChEMBL 靶标：Mycobacterium tuberculosis External Id：CHEMBL4774839

实验名称：Cytotoxicity against human U2OS cells expressing tetracyclin/Dox-inducible N-terminal... 来源：ChEMBL 靶标：U2OS External Id：CHEMBL5337153

实验名称：A screen for small molecules that modulate mitochondrial supercomplex formation 来源：ICCB-Longwood/NSRB Screening Facility, Harvard Medical School 靶标：N/A External Id：HMS1482

实验名称：Inhibition of tetracyclin/Dox-inducible N-terminal 3xFLAG/C-terminal GFP tagged human... 来源：ChEMBL 靶标：Methylcytosine dioxygenase TET1 External Id：CHEMBL5337152

实验名称：Cell-based high throughput primary assay to identify activators of GPR151 来源：The Scripps Research Institute Molecular Screening Center 靶标：RecName: Full=G-protein coupled receptor 151; AltName: Full=G-protein coupled receptor PGR7; AltName: Full=GPCR-2037; AltName: Full=Galanin receptor 4; AltName: Full=Galanin-receptor-like protein; Short=GalRL External Id：GPR151_PHUNTER_AG_LUMI_1536_1X%ACT

实验名称：AlphaScreen-based biochemical high throughput primary assay to identify inhibitors of... 来源：The Scripps Research Institute Molecular Screening Center External Id：MITF_INH_Alpha_1536_1X%INH PRUN

实验名称：Solubility of compound in water 来源：ChEMBL 靶标：N/A External Id：CHEMBL4774863

实验名称：Stabilization of p53 in human papillomavirus-positive cells 来源：ICCB-Longwood/NSRB Screening Facility, Harvard Medical School 靶标：Cellular tumor antigen p53 External Id：HMS1485

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4-氧代-1,4-二氢-1,10-菲咯啉-3-羧酸英文别名

• T B666 CN NNJ EVQ FQ
• 1,4-Dihydro-4-oxo-1,10-phenanthroline-3-carboxylic acid
• 4-Hydroxy-1,10-phenanthroline-3-carboxylic acid
• T B666 CM FV NNJ EVQ
• 4-Oxo-1,4-dihydro-1,10-phenanthroline-3-carboxylic acid
• 4-Oxo-1,4-dihydro-[1,10]phenanthroline-3-carboxylic acid
• 1,4-dpca
• MFCD07357380