苏拉明钠
| 中文名称 | 苏拉明钠 |
|---|---|
| 中文同义词 | 苏拉明钠(SURAMIN);8,8'-碳酰双亚氨-3,1-亚苯基碳酰亚氨-(4-甲基-3,1-亚苯基)碳酰亚氨双-1,3,5-萘三磺酸六钠;苏拉明钠;苏拉明钠盐;蘇拉明鈉;苏拉明;舒拉明钠;苏拉林 |
| 英文名称 | Suramin sodium |
| 英文同义词 | naphuridesodium;nf060;reasodiumsalt;sodiumsuramin;suraminesodium;SURAMIN;SURAMIN SODIUM, 98+%;8,8'-[Carbonylbis[imino-3,1-phenylenecarbonylimino(4-methyl-3,1-phenylene)carbonylimino]]bis-1,3,5-naphthalenetrisulfoni |
| CAS号 | 129-46-4 |
| 分子式 | C51H34N6Na6O23S6 |
| 分子量 | 1429.17 |
| EINECS号 | 204-949-3 |
| 相关类别 | 小分子抑制剂，天然产物;合成;小分子抑制剂;细胞生物学试剂;医药原料;原料;化工原料;杂质对照品;试剂盒-细胞分析试剂盒;Inhibitors;Active Pharmaceutical Ingredients;Purinergics P2 receptor;EPIVIR |
| Mol文件 | 129-46-4.mol |
| 结构式 |  |
苏拉明钠 性质
| 熔点 | >260°C (dec.) |
|---|---|
| 储存条件 | 0-6°C |
| 溶解度 | H2O:>10mg/mL |
| 形态 | 结晶粉末 |
| 颜色 | 白色 |
| PH值 | pH(10g/l, 25℃) : 5.0～8.0 |
| 水溶解性 | soluble |
| BRN | 3694087 |
| 稳定性 | 吸湿性 |
| InChIKey | VAPNKLKDKUDFHK-UHFFFAOYSA-H |
苏拉明钠是一种可逆的竞争性蛋白酪氨酸磷酸酶 (PTPases) 抑制剂。苏拉明钠是有效的 sirtuins 抑制剂：SirT1 (IC50=297 nM)，SirT2 (IC50=1.15 μM)，SirT5 (IC50=22 μM)。苏拉明钠是竞争性逆转录酶抑制剂 (DNA topoisomerase II: IC50=5 μM)。苏拉明钠有效抑制 IP5K，并且是抗寄生虫 (antiparasitic)，抗肿瘤和抗血管生成剂。
苏拉明钠已经被证实具有抗锥虫病，抗肿瘤，防治眼部增殖性疾病，抗病毒，免疫调节剂的作用，并广泛应用于临床实践中。目前尚未有苏拉明钠具有抗鸡球虫作用的报导，通过苏拉明钠已知的性质无法推断其是否具有抗鸡球虫的作用。
苏拉明钠盐，是一种丙型肝炎病毒 NS3 解旋酶抑制剂。 也用于治疗因胶原蛋白问题引起的关节炎。
|
SIRT1 297 nM (IC 50 ) |
SIRT2 1.15 μM (IC 50 ) |
SIRT5 22 μM (IC 50 ) |
Suramin sodium salt (Suramin hexasodium salt; 50-600 μg/mL; for 24-96 hours) inhibits cells proliferation in a dose-dependent and time-dependent manner and decreases viability in cancer cells.
Suramin sodium salt (300 μg/mL; for 48 hours) induces cells apoptosis and down-regulates mRNA expression in HeLa cells.
Suramin sodium salt (1 mg/mL; 1 hour) significantly suppresses the phosphorylated ERK1/2.
The IC
50
values of HO-8910 PM and HeLa are 319 μg/mL, 476 μg/mL, respectively.
Suramin blocks viral replication in Vero E6 cells.
Cell Proliferation Assay
| Cell Line: | HO-8910 PM ovarian and Hela cervical cancer cells |
| Concentration: | 50, 100, 200, 300, 400, 500 and 600 μg/mL |
| Incubation Time: | For 24, 48, 72 and 96 hours |
| Result: | Inhibited cells proliferation in a dose-dependent and time-dependent manner. |
Apoptosis Analysis
| Cell Line: | HeLa cells |
| Concentration: | 300 μg/mL |
| Incubation Time: | For 48 hours |
| Result: | Induced cells apoptosis. |
Western Blot Analysis
| Cell Line: | PA-SMCs cells |
| Concentration: | 1 mg/mL |
| Incubation Time: | For 1 hour |
| Result: | Significantly suppressed the phosphorylated ERK1/2. |
Suramin sodium salt (Suramin hexasodium salt; 10 mg/kg; IV; twice weekly for 3 weeks) reverses established pulmonary hypertension (PH), thereby normalizing the pulmonary artery pressure values and vessel structure.
| Animal Model: | Adult male Wistar rats (200-225 g) |
| Dosage: | 10 mg/kg |
| Administration: | IV; twice weekly for 3 weeks |
| Result: | Reversed established PH, thereby normalizing the pulmonary artery pressure values and vessel structure. |
安全信息
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