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化驗
≥97% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: ≥5 mg/mL
儲存溫度
room temp
SMILES 字串
C(c1ccccc1)n2nnc3c(Sc4nc5ccccc5o4)ncnc23
InChI
1S/C18H12N6OS/c1-2-6-12(7-3-1)10-24-16-15(22-23-24)17(20-11-19-16)26-18-21-13-8-4-5-9-14(13)25-18/h1-9,11H,10H2
InChI 密鑰
HZSOKHVVANONPV-UHFFFAOYSA-N
應用
使用 VAS2870 作为烟酰胺腺嘌呤二核苷酸磷酸(NADPH)氧化酶(NOX)的抑制剂:
- 研究 NOX 衍生的活性氧簇在斑马鱼表皮生长过程中细胞骨架组织、上皮细胞钙粘蛋白的正确定位和细胞运动中的重要性
- 研究 Nox2 和 Nox4 在高脂饮食(HFD)喂养小鼠的脂多糖(LPS)诱导肠道损伤中的作用
- 降低单核细胞活性氧水平并研究其对抑制训练型先天免疫诱导的影响
生化/生理作用
VAS2870 是一种细胞渗透性特异性 NADPH 氧化酶(NOX)抑制剂,可有效抑制血管平滑肌细胞(VSMC)中生长因子介导的 ROS 释放。
除了能抑制 NOX4 之外,VAS2870 还可抑制多种类型细胞中活性氧簇(ROS)的产生。它可有效地抑制肝癌细胞的生长,增加转化生长因子β(TGF β)诱导的细胞凋亡。因此,通过 VAS2870 抑制 NOX 酶可能成为一种潜在的肝癌治疗方案。
儲存類別代碼
11 - Combustible Solids
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
Frontiers in immunology, 9, 3155-3155 (2019-02-07)
Introduction: Cells of the innate immune system particularly monocytes and macrophages have been recognized as pivotal players both during the initial insult as well as the chronic phase of atherosclerosis. It has recently been shown that oxidized low-density lipoprotein (oxLDL)
Free radical biology & medicine, 52(9), 1897-1902 (2012-03-13)
Specific inhibitors of the production of reactive oxygen species (ROS) by the NADPH oxidases (Nox's) are potentially important therapeutic agents in the wide range of human diseases that are characterized by excessive ROS production. It has been proposed that VAS2870
Biochemical pharmacology, 81(7), 917-924 (2011-02-01)
Liver tumor cells show several molecular alterations which favor pro-survival signaling. Among those, we have proposed the NADPH oxidase NOX1 as a prosurvival signal for liver tumor cells. On the one side, we have described that FaO rat hepatoma cells
American journal of physiology. Heart and circulatory physiology, 312(5), H896-H906 (2017-02-27)
High blood pressure has been shown to elicit impaired dilation in the vasculature. The purpose of this investigation was to elucidate the mechanisms through which high pressure may elicit vascular dysfunction and determine the mechanisms through which regular aerobic exercise
Biochimica et biophysica acta. Molecular basis of disease, 1864(11), 3792-3804 (2018-09-27)
Low concentrations of cardiac glycosides including ouabain, digoxin, and digitoxin block cancer cell growth without affecting Na+,K+-ATPase activity, but the mechanism underlying this anti-cancer effect is not fully understood. Volume-regulated anion channel (VRAC) plays an important role in cell death
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