所有图片(1)
别名:
2,5-双（4-脒基苯基）呋喃 二盐酸盐, 4,4′-（2,5-呋喃二基）二苯甲酰胺 二盐酸盐, DB 75, DB75, NSC 305831, WR199385
经验公式（希尔记法）:
C18H16N4O · 2HCl
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质量水平
检测方案
≥98% (HPLC)
形式
powder
储存条件
desiccated
颜色
white to beige
溶解性
H2O: 1 mg/mL, clear (warmed)
储存温度
−20°C
InChI
1S/C18H16N4O.2ClH/c19-17(20)13-5-1-11(2-6-13)15-9-10-16(23-15)12-3-7-14(8-4-12)18(21)22;;/h1-10H,(H3,19,20)(H3,21,22);2*1H
InChI key
VXNYQUQHOUERTR-UHFFFAOYSA-N
一般描述
呋喃脒二盐酸盐是芳香族药物喷他脒的类似物，也是有机阳离子转运蛋白 1 (OCT1) 的底物。编号呋喃脒二盐酸盐的前体药物正在合成并处于临床试验阶段。
生化/生理作用
呋喃脒 (DB75) 与 DNA 小槽中与 AT 碱基对序列结合。呋喃脒最初作为抗寄生虫化合物开发，用于多种疾病，包括恰加斯病。呋喃脒类的靶点是锥体虫微环 DNA (kDNA) 中的丰富序列，导致动基体的破坏和细胞死亡。呋喃脒也被发现可以抑制酪氨酰-DNA 磷酸二酯酶 (Tdp1) ，并作为一种选择性蛋白质精氨酸甲基转移酶 1 (PRMT1) 抑制剂 ，IC 50 为 9.4 μmol/l。M.
WGK
WGK 3
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The antiparasitic activity of aromatic diamidine drugs, pentamidine and furamidine, depends on their entry into the pathogenic protozoa via membrane transporters. However, no such diamidine transporter has been identified in mammalian cells. The goal of this study is to investigate
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Wilson
Biochimie, 90(7), 999-1014 (2008)
Leilei Yan et al.
Journal of medicinal chemistry, 57(6), 2611-2622 (2014-02-26)
Protein arginine methylation is a posttranslational modification critical for a variety of biological processes. Misregulation of protein arginine methyltransferases (PRMTs) has been linked to many pathological conditions. Most current PRMT inhibitors display limited specificity and selectivity, indiscriminately targeting many methyltransferase
Yang Liu et al.
The journal of physical chemistry. B, 112(37), 11809-11818 (2008-08-23)
Given the increasing significance of diamidines as DNA-targeted therapeutics and biotechnology reagents, it is important to establish the variations in thermodynamic quantities that characterize the interactions of closely related compounds to different sequence AT binding sites. In this study, an
Smitha Antony et al.
Nucleic acids research, 35(13), 4474-4484 (2007-06-20)
By enzymatically hydrolyzing the terminal phosphodiester bond at the 3'-ends of DNA breaks, tyrosyl-DNA phosphodiesterase (Tdp1) repairs topoisomerase-DNA covalent complexes and processes the DNA ends for DNA repair. To identify novel Tdp1 inhibitors, we developed a high-throughput assay that uses
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