苏拉明钠
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 用途与合成方法
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
安全说明 | 22-24/25 |
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WGK Germany | 3 |
RTECS号 | QM7000000 |
F | 3-10 |
海关编码 | 29242998 |
毒性 | LD50 in mice (mg/kg): ~620 i.v. (Hawking) |
苏拉明钠 价格(试剂级)
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
---|---|---|---|---|---|
2024-11-08 | 32854 | 苏拉明钠 | 129-46-4 | 50mg | 2250 |
2024-11-08 | HY-B0879A | 苏拉明钠 | 129-46-4 | 25mg | 2100 |