GlpBio

VAS2870

目录号: GC32443纯度: >98.50%

A pan-NADPH oxidase inhibitor

VAS2870
Cas No.: 722456-31-7
规格价格库存数量操作
1mg¥270.00现货
1
5mg¥593.00现货
1
10mg¥1,035.00现货
1
25mg¥1,980.00现货
1
50mg¥3,555.00现货
1
100mg¥5,104.00现货
1
10mM (in 1mL DMSO)¥653.00现货
1
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文献被引

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产品描述 Description

VAS2870 is a selective inhibitor of the NADPH oxidases.1,2,3,4 Pre-incubation of rat vascular smooth muscle cells with VAS2870 abolishes platelet-derived growth factor-dependent chemotaxis without affecting cell cycle progression (IC50 = 10 ?M).1 At low (2.8 mM), but not high (16.7 mM), concentrations of glucose, treatment with VAS2870 (20 ?M) increases glucose-stimulated insulin secretion of rat pancreatic islets by 70%.5 It significantly reduces production of reactive oxygen species in mouse brain, rat vascular smooth muscle culture, and human umbilical vein endothelial cells.1,6,7 Treatment with VAS2870 pre- or post-ischemia is neuroprotective in mouse brain.6 VAS2870 inhibits vasculogenesis of mouse embryonic stem cell cultures and inhibits cell proliferation of rat hepatoma cells.8,9

1.ten Freyhaus, H., Huntgeburth, M., Wingler, K., et al.Novel Nox inhibitor VAS2870 attenuates PDGF-dependent smooth muscle cell chemotaxis, but not proliferationCardiovasc. Res.71(2)331-341(2006) 2.Altenh?fer, S., Kleikers, P.W.M., Radermacher, K.A., et al.The NOX toolbox: validating the role of NADPH oxidases in physiology and diseaseCell. Mol. Life Sci.69(14)2327-2343(2012) 3.Wingler, K., Altenhofer, S.A., Kleikers, P.W.M., et al.VAS2870 is a pan-NADPH oxidase inhibitorCell. Mol. Life Sci.69(18)3159-3160(2012) 4.Wind, S., Beuerlein, K., Eucker, T., et al.Comparative pharmacology of chemically distinct NADPH oxidase inhibitorsBr. J. Pharmacol.161(4)885-898(2010) 5.Munhoz, A.C., Riva, P., Sim?es, D., et al.Control of insulin secretion by production of reactive oxygen species: Study performed in pancreatic islets from fed and 48-hour fasted Wistar ratsPLoS One11(6)e0158166(2016) 6.Kleinschnitz, C., Grund, H., Wingler, K., et al.Post-stroke inhibition of induced NADPH oxidase type 4 prevents oxidative stress and neurodegenerationPLoS One8(9)e1000479(2010) 7.Stielow, C., Catar, R.A., Muller, G., et al.Novel Nox inhibitor of oxLDL-induced reactive oxygen species formation in human endothelial cellsBiochem. Biophys. Res. Commun.344(1)200-205(2006) 8.Lange, S., Heger, J., Euler, G., et al.Platelet-derived growth factor BB stimulates vasculogenesis of embryonic stem cell-derived endothelial cells by calcium-mediated generation of reactive oxygen speciesCardiovasc. Res.81(1)159-168(2009) 9.Sancho, P., and Fabregat, I.The NADPH oxidase inhibitor VAS2870 impairs cell growth and enhances TGF-β-induced apoptosis of liver tumor cellBiochem. Pharmacol.81(7)917-924(2011)

实验参考方法 Experimental Reference Method

Kinase experiment:

NADPH oxidase activity is measured by lucigenin-enhanced chemiluminescence in a 50 mM phosphate buffer (buffer A), pH 7.0, containing 1 mM EGTA, protease inhibitors, 150 mM sucrose, 5 μM lucigenin, and 250 μM NADPH as substrate. Quiescent cells are starved by serum deprivation for 24 h and treated as indicated, ished twice with ice-cold phosphate buffered saline (PBS), pH 7.4, and harvested. After low spin centrifugation, the pellet is re-suspended in ice-cold buffer A, lacking lucigenin and substrate. Then, the cells are lysed and total protein concentration is determined using a Bradford assay and adjusted to 1 mg/mL. 100 μL aliquots of the protein sample are measured over 6 min in quadruplicates using NADPH (100 μM) as substrate in a scintillation counter. Data are collected at 2 min intervals in order to measure relative changes in NADPH oxidase activity[1].

Cell experiment:

To test autocrine growth, cells are serum deprived at 40% confluence and, when indicated, the NADPH oxidase inhibitors Apocynin (300 mM) or VAS2870 are added 30 min before serum deprivation and maintained along the experiment. For TGF-b experiments, cells at 70% confluence are serum deprived for 16 h and treated with 2 ng/mL TGF-β in the presence or absence of the EGFR inhibitor AG1478 (20 mM) or VAS2870 (25 mM), which are added 30 min prior to TGF-β[2].

References:

[1]. ten Freyhaus H, et al. Novel Nox inhibitor VAS2870 attenuates PDGF-dependent smooth muscle cell chemotaxis, but not proliferation. Cardiovasc Res. 2006 Jul 15;71(2):331-41.
[2]. Sancho P, et al. The NADPH oxidase inhibitor VAS2870 impairs cell growth and enhances TGF-β-induced apoptosis of liver tumor cells. Biochem Pharmacol. 2011 Apr 1;81(7):917-24.

产品文档 Product Documents

Purity:>98.50%

化学性质Chemical Properties

CAS 号
722456-31-7
SMILES
C1(N(CC2=CC=CC=C2)N=N3)=C3C(SC4=NC5=C(C=CC=C5)O4)=NC=N1
分子式
C18H12N6OS
分子量
360.39 g/mol
溶解性
DMSO : 83.3 mg/mL (231.14 mM)
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol