145-63-1
145-63-1 結構式
基本信息
蘇拉滅
舒拉明
Fourneau
Suramine
Naphuride
Farma 939
Aids000067
Aids-000067
129-46-4(Hexasodium salt)
8,8-[carbonylbis[imino-3,1-phenylenecarbonylimino(4-methyl-3,1-phenylene)carbonylimino]]bisnaphthalene-1,3,5-trisulphonic acid
8,8'-[Carbonylbis[imino-3,1-phenylenecarbonylimino(4-methyl-3,1-phenylene)carbonyl-imino]]bis-1,3,5-naphthalenetrisulfonic acid
物理化學性質
常見問題列表
|
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. |