Potassium bisperoxo(1,10-phenanthroline)oxovanadate(V) | 42494-73-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 菲咯啉
• 英文名称: Potassium bisperoxo(1,10-phenanthroline)oxovanadate(V)
• 英文别名: potassium;oxovanadium;1,10-phenanthroline-1,10-diide;diperoxide
• CAS: 42494-73-5
• 化学式: C12H8KN2O5V-5
• 分子量: 350.24
• InChiKey: LXOJIFVIHKEULW-UHFFFAOYSA-N

物化性质

• 溶解度：
  在水中的溶解度为20mg/mL，澄清

计算性质

• 辛醇/水分配系数(LogP)：
  -5.56
• 重原子数：
  21
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  111
• 氢给体数：
  0
• 氢受体数：
  7

制备方法与用途

生物活性

bpV(phen)，一种胰岛素模拟物，是一种有效的蛋白酪氨酸磷酸酶 (PTP) 和 PTEN 抑制剂，对 PTEN，PTP-β 和 PTP-1B 的 IC50 为 38 nM，343 nM 和 920 nM。bpV(phen) 在体外抑制原生动物寄生虫利什曼原虫的增殖。bpV(phen) 强烈诱导大量趋化因子和促炎性细胞因子的分泌，并激活 Th1 型途径 (IL-12，IFNγ)。bpV(phen) 还可以诱导细胞凋亡 (apoptosis)，并具有抗血管生成和抗肿瘤活性。

靶点

IC50: 38 nM (PTEN), 343 nM (PTP-β) and 920 nM (PTP-1B)
Parasite Leishmania
Apoptosis

体外研究

bpV(phen) (5 μM; 24.5 hours; H9c2 cells) treatment causes a further decrease of cell viability in H/R-injured H9c2 cells.
bpV(phen) (5 μM; 24.5 hours; H9c2 cells) treatment increases the apoptosis of H/R-injured H9c2 cells.
bpV(phen) (5 μM; 24.5 hours; H9c2 cells) treatment significantly promotes the accumulation of cytoplasmic Cytochrome C in H/R-injured H9c2 cells.
After stimulation of bpV(phen), PTEN-induced putative kinase protein 1 (PINK1)/Parkin-mediated mitophagy is inhibited.
bpV(phen) is an insulin-mimetic agent following insulin-receptor tyrosine kinase hyperphosphorylation and activation.

Cell Viability Assay

Cell Line:	Hypoxia/reoxygenation (H/R)-injured H9c2 cells
Concentration:	5 μM
Incubation Time:	24.5 hours (hypoxia for 24 h; reoxygenation for 30 minutes)
Result:	Caused a further decrease of cell viability.

Apoptosis Analysis

Cell Line:	Hypoxia/reoxygenation (H/R)-injured H9c2 cells
Concentration:	5 μM
Incubation Time:	24.5 hours (hypoxia for 24 h; reoxygenation for 30 minutes)
Result:	Increased the apoptosis of H/R-injured H9c2 cells.

Western Blot Analysis

Cell Line:	Hypoxia/reoxygenation (H/R)-injured H9c2 cells
Concentration:	5 μM
Incubation Time:	24.5 hours (hypoxia for 24 h; reoxygenation for 30 minutes)
Result:	Showed an increased release of Cytochrome C.

体内研究

bpV(phen) (5 mg/kg; intraperitoneal injection; daily; for 38 days; male BALB/c nude (nu/nu) athymic mice) treatment causes a significant reduction in average tumor volume.

Animal Model:	Male BALB/c nude (nu/nu) athymic mice (6-7 weeks old) injected with PC-3 cells
Dosage:	5 mg/kg
Administration:	Intraperitoneal injection; daily; for 38 days
Result:	Caused a significant reduction in average tumor volume.