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23256-30-6

中文名称 硝呋替莫
英文名称 nifurtimox
CAS 23256-30-6
分子式 C10H13N3O5S
分子量 287.295
MOL 文件 23256-30-6.mol
更新日期 2025/05/12 14:07:39
23256-30-6 结构式 23256-30-6 结构式

基本信息

中文别名
硝呋替莫
NIFURTIMOX [4-氨基-3-甲基四氢-1,4-噻嗪-1,1-二氧化物]
英文别名
Lampit
BAY-2502
NIFURIMOX
Bayer-2502
Bayer 2502
Aids007325
nifurtimox
BAY-A-2502
Aids-007325
nifurtimox USP/EP/BP
所属类别
生物化工:酶及辅酶类

物理化学性质

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Refrigerator
溶解度在DMSO中的溶解度≥13mg/mL
酸度系数(pKa)-1.01±0.40(Predicted)
形态粉末
颜色黄色到橙色
水溶解性33g/L(temperature not stated)
BCS Class3
InChIKeyARFHIAQFJWUCFH-IZZDOVSWSA-N

安全数据

危险性符号(GHS)GHS hazard pictograms
GHS08
警示词警告
危险性描述H373
防范说明P260-P314-P501
WGK Germany3
毒性LD50 in mice, rats (mg/kg): 3720, 4050 by gavage (Hoffmann)

常见问题列表

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.

硝呋替莫价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2025/02/08HY-W040073硝呋替莫
Nifurtimox
23256-30-65mg800元
2025/02/08HY-W040073硝呋替莫
Nifurtimox
23256-30-610mM * 1mLin DMSO880元
2025/02/08HY-W040073硝呋替莫
Nifurtimox
23256-30-610mg1280元
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