1-亚硝基-2-萘酚-6-磺酸钠铁盐; 1-亚硝基-2-萘酚铁色淀; 媒染草绿; 酸性绿O; 萘酚绿B; 酸性绿1; 颜料绿; 三[5,6-二氢-5-(羟基亚氨)-6-氧代-2-萘磺酸(2-)-N5,O6]铁酸(III)三钠; 绿色染料; trisodium iron(3+) 5-nitroso-6-oxidonaphthalene-2-sulfonate; Ext D and C Green No. 1; C.I. Acid Green 1; D and C Green 1; Acid green 1; Naphthol Green; C.I. Pigment Green 12; C Green 1
- 生物活性
SKA-31 是钾离子通道 (potassium channel) 激活剂，作用于 KCa3.1，KCa2.2，KCa2.1 和 KCa2.3 的 EC50 值分别为 260 nM，1.9 μM，2.9 μM，2.9 μM，能增强内皮源性超极化因子反应，降低血压。
- 靶点
EC50: 2.9 μM (KCa2.1), 1.9 μM (KCa2.2), 2.9 μM (KCa2.3), 260 nM (KCa3.1)
- 体外研究
SKA-31 activates KCa2/3 channels more potently than PK 26124, and is more selective over other Ion channels.
SKA-31 reduces cell viability with IC
50s
of 5.3 μM , 46.9 μM in HCT-116 cells and HCT-8 cells, respectively.
SKA-31 (5.3 μM; 0-96 hours) reduces HCT-116 cells proliferation when added at time zero at 5.3 μM.
SKA-31 triggers apoptosis in HCT-116 cells at 5 μM, and the effect is smaller in HCT-8 cells at 45 μM.
SKA-31 increases the percentage of cells in G0/G1 phase in HCT-116 and HCT-8 cell lines at 5 μM and 45 μM, respectively.
SKA-31 further activates Caspase 3 and reduces Akt phosphorylation induced by CDDP.
SKA-31 has a synergic effect with CDDP also on the inhibition of HCT-116 cell proliferation.
Cell Viability Assay
Cell Line:
HCT-116 cells, HCT-8 cells
Concentration:
Incubation Time:
24 hours
Result:
Reduced cell viability with IC
50s
of 5.3 μM , 46.9 μM in HCT-116 and HCT-8, respectively.
Cell Proliferation Assay
Cell Line:
HCT-116 cells
Concentration:
5.3 μM
Incubation Time:
0-96 hours
Result:
Reduced HCT-116 cells proliferation when added at time zero at IC
50S
value.
Apoptosis Analysis
Cell Line:
HCT-116 cells, HCT-8 cells
Concentration:
5 μM (HCT-116 cells), 45 μM (HCT-8 cells)
Incubation Time:
24 hours
Result:
Triggered apoptosis in HCT-116 cells, and the effect was smaller in HCT-8 cells.
Cell Cycle Analysis
Cell Line:
HCT-116 cells, HCT-8 cells
Concentration:
5 μM (HCT-116), 45 μM (HCT-8)
Incubation Time:
24 hours
Result:
Increased the percentage of cells in G0/G1 phase in HCT-116 and HCT-8 cell lines.
Western Blot Analysis
Cell Line:
HCT-116 cells
Concentration:
Incubation Time:
24 hours
Result:
Further activated Caspase 3 and reduced Akt phosphorylation when co-treatment with CDDP in HCT-116 cells.
- 体内研究
SKA-31 is not acutely toxic and has good pharmacokinetic properties.
SKA-31 potentiates native KCa3.1 and KCa2.3 in murine carotid endothelium with EC
50
values of 225 nM and 1.6 μM for KCa3.1 and KCa2.3, respectively.
SKA-31 stimulates KCa3.1 and KCa2.3 in vascular endothelial cells and increases acetylcholine-induced endothelium-derived hyperpolarizing factor (EDHF) -mediated vasodilation.
SKA-31 potentiates EDHF-type vasodilations and lowers blood pressure in mice. Injections of SKA-31 (1-30 mg/kg; i.p.) lower MAP over 24 hours in normotensive wild-type mice but not in KCa3.1(-/-) mice (-/-).
Animal Model:
16-25 weeks mice
Dosage:
1 mg/kg, 10 mg/kg, and 30 mg/kg
Administration:
Intraperitoneal injection
Result:
Lower MAP over 24 hours in normotensive wild-type mice but not in KCa3.1(-/-) mice (-/-).
