硝呋替莫
| 中文名称 | 硝呋替莫 |
|---|---|
| 中文同义词 | NIFURTIMOX [4-氨基-3-甲基四氢-1,4-噻嗪-1,1-二氧化物];硝呋替莫;硝呋莫司;3-甲基-4-(((5-硝基呋喃-2-基)亚甲基)氨基)硫代吗啉 1,1-二氧化物 |
| 英文名称 | nifurtimox |
| 英文同义词 | NIFURIMOX;4-[(5-Nitrofurfurylidene)amino]-3-methylthiomorpholine 1,1-dioxide;BAY-2502;Bayer 2502;Bayer-2502;Lampit;3-Methyl-N-[(5-nitro-2-furanyl)methylene]-4-thiomorpholinamine 1,1-dioxide;Aids007325 |
| CAS号 | 23256-30-6 |
| 分子式 | C10H13N3O5S |
| 分子量 | 287.29 |
| EINECS号 | 245-531-0 |
| 相关类别 | Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;Sulfur & Selenium Compounds |
| Mol文件 | 23256-30-6.mol |
| 结构式 |  |
硝呋替莫 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 | 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 | 黄色至橙色粘性至蜡状 |
| 水溶解性 | 33g/L(temperature not stated) |
| BCS Class | 3 |
| InChIKey | ARFHIAQFJWUCFH-IZZDOVSWSA-N |
Trypanosoma cruzi
Lactate dehydrogenase (LDH)
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.
安全信息
| WGK Germany | 3 |
|---|---|
| 毒性 | LD50 in mice, rats (mg/kg): 3720, 4050 by gavage (Hoffmann) |
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-W040073 | 硝呋替莫 Nifurtimox | 23256-30-6 | 5mg | 800元 |
| 2024/01/25 | HY-W040073 | 硝呋替莫 Nifurtimox | 23256-30-6 | 10mM * 1mLin DMSO | 880元 |