SURAMIN

SURAMIN

中文名称SURAMIN
中文同义词舒拉明;苏拉灭;苏拦明
英文名称8,8'-[carbonylbis[imino-3,1-phenylenecarbonylimino(4-methyl-3,1-phenylene)carbonylimino]]bisnaphthalene-1,3,5-trisulphonic acid
英文同义词8,8'-[carbonylbis[imino-3,1-phenylenecarbonylimino(4-methyl-3,1-phenylene)carbonylimino]]bisnaphthalene-1,3,5-trisulphonic acid;Farma 939;Fourneau;Naphuride;Suramine;129-46-4(Hexasodium salt);8,8'-[Carbonylbis[imino-3,1-phenylenecarbonylimino(4-methyl-3,1-phenylene)carbonyl-imino]]bis-1,3,5-naphthalenetrisulfonic acid;Aids000067
CAS号145-63-1
分子式C51H40N6O23S6
分子量1297.28
EINECS号205-658-4
相关类别
Mol文件145-63-1.mol
结构式SURAMIN 结构式

SURAMIN 性质

熔点128 °C(Solv: ethyl ether (60-29-7))
密度1.2629 (rough estimate)
折射率1.7770 (estimate)
储存条件Store at -20°C
溶解度溶于二甲基亚砜
酸度系数(pKa)-1.35±0.40(Predicted)
颜色粉白色吸湿性粉末
EPA化学物质信息Suramin (145-63-1)

SURAMIN 用途与合成方法

Suramin 是一种可逆的,竞争性蛋白酪氨酸磷酸酶 (PTPases) 抑制剂。Suramin 是有效的 sirtuins 抑制剂:SirT1 (IC50=297 nM),SirT2 (IC50=1.15 μM),SirT5 (IC50=22 μM)。Suramin 是竞争性逆转录酶抑制剂 (DNA topoisomerase II: IC50=5 μM)。Suramin 是一种有效的 SARS-CoV-2 RNA 依赖性 RNA 聚合酶 (RdRp) 抑制剂。Suramin 有效抑制 IP5K,并且是抗寄生虫 (antiparasitic),抗肿瘤和抗血管生成剂。

SIRT1

297 nM (IC 50 )

SIRT2

1.15 μM (IC 50 )

SIRT5

22 μM (IC 50 )

Suramin (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 (300 μg/mL; for 48 hours) induces cells apoptosis, and down-regulates mRNA expression in HeLa cells.
Suramin (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 hours
Result: Significantly suppressed the phosphorylated ERK1/2.

Suramin (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.
类别
有毒物品
毒性分级
中毒
急性毒性
静脉-小鼠 LD50: 620 毫克/公斤
可燃性危险特性
可燃; 燃烧产生有毒氮氧化物和硫氧化物烟雾
储运特性
通风低温干燥
灭火剂
干粉,泡沫,沙土,二氧化碳, 雾状水

安全信息

毒性LD50 intravenous in mouse: 620mg/kg

MSDS信息

SURAMIN 上下游产品信息

"SURAMIN"相关产品信息
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