硝呋替莫

应用作用生物活性靶点体外研究硝呋替莫试剂级价格

硝呋替莫

CAS号:23256-30-6
英文名:nifurtimox
中文名:硝呋替莫
CBNumber:CB3903922
分子式:C10H13N3O5S
分子量:287.29
MOL File:23256-30-6.mol

硝呋替莫化学性质

熔点 :177-183°C
沸点 :550.3±50.0 °C(Predicted)
密度 :1.4716 (rough estimate)
折射率 :1.6390 (estimate)
储存条件 :room temp
溶解度 :DMSO: ≥13mg/mL
酸度系数(pKa) :-1.01±0.40(Predicted)
形态 :powder
颜色 :yellow to orange
水溶解性 :33g/L(temperature not stated)
BCS Class :3
InChIKey :ARFHIAQFJWUCFH-IZZDOVSWSA-N

安全信息

WGK Germany :3
毒性 :LD50 in mice, rats (mg/kg): 3720, 4050 by gavage (Hoffmann)

硝呋替莫性质、用途与生产工艺

应用硝呋替莫是现在几乎唯一的对这些病原体具有活性的化合物。该活性可能是基于对酶Trypanothione还原酶(一种特殊的锥虫酶)的抑制。这种酶在其他原生动物病原体中是不存在的。
作用硝呋替莫（nifurtimox）是自20世纪70年代以来治疗南美锥虫病（Chagasdisease）的主要药物，为一种硝基杂环类化合物，在细胞内被还原成硝基阴离子自由基、过氧化氢和超氧化物自由基等活性氧（reactiveoxygenspecies，ROS）。硝呋替莫和其他硝基呋喃化合物能够用于治疗癌症和由血管发生所介导或引起的疾病或病症。
生物活性 Nifurtimox (BAY-2502) 是一种抗原虫剂。
靶点

Trypanosoma cruzi
Lactate dehydrogenase (LDH)
体外研究

Nifurtimox affects enzyme activity of lactate dehydrogenase (LDH). To differentiate if this effect is a result of a reduced LDH activity or a shift in pyruvate metabolism due to activation of PDH, the enzyme activity of LDH is determined after 4 h treatment with 50 µg/mL Nifurtimox. Compared to the untreated control, the LDH activity is significantly reduced for LA-N-1 (P=0.005), IMR-32 (P=0.009), LS (P=0.0035) and SK-N-SH (P=0.0065). Nifurtimox reduces cell viability and induces cell cycle arrest and apoptosis in neuroblastoma cells. To characterize the cytotoxic impacts of Nifurtimox on neuroblastoma, 4 cell lines are subjected to several experiments. Cell viability is reduced for all 4 neuroblastoma cell lines after 24 h incubation with 50 µg/mL to an average of 66%, 63%, 62% and 75% (LA-N-1, IMR-32 LS and SK-N-SH, respectively). The reduction is significant compared to the untreated control (P<0.01) and the vehicle control with DMSO (P<0.05) for all cell lines.