VAS2870
目录号 : GC32443
A pan-NADPH oxidase inhibitor
Cas No.:722456-31-7
Sample solution is provided at 25 µL, 10mM.
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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)
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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]. |
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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]. |
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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. |
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| Cas No. | 722456-31-7 | SDF | |
| Canonical 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 |
| 溶解度 | DMSO : 83.3 mg/mL (231.14 mM) | 储存条件 | 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℃，然后在超声波浴中震荡一段时间。 |
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| 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。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7748 mL | 13.8739 mL | 27.7477 mL |
| 5 mM | 0.555 mL | 2.7748 mL | 5.5495 mL |
| 10 mM | 0.2775 mL | 1.3874 mL | 2.7748 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet