722456-31-7
722456-31-7 structure
- Name: VAS 2870
- Chemical Name: VAS2870
- CAS Number: 722456-31-7
- Molecular Formula: C18H12N6OS
- Molecular Weight: 360.392
- Catalog: Research Areas Cardiovascular Disease
- Create Date: 2018-06-30 16:20:48
- Modify Date: 2024-01-13 11:42:32
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VAS2870 is a NADPH oxidase (NOX) inhibitor.
| Name | VAS2870 |
|---|---|
| Synonyms |
3-benzyl-7-(2-benzoxazolyl)thio-1,2,3-triazolo(4,5-d)pyrimidine
Benzoxazole, 2-[[3-(phenylmethyl)-3H-1,2,3-triazolo[4,5-d]pyrimidin-7-yl]thio]- 7-(1,3-Benzoxazol-2-ylsulfanyl)-3-benzyl-3H-[1,2,3]triazolo[4,5-d]pyrimidine |
| Description | VAS2870 is a NADPH oxidase (NOX) inhibitor. |
|---|---|
| Related Catalog | |
| Target |
Target: NADPH oxidase[1] |
| In Vitro | VAS2870 is effective to suppress PDGF-BB-dependent activation of NADPH oxidase and subsequent production of intracellular ROS. Furthermore, VAS2870 suppresses PDGF-BB-dependent chemotaxis, but not DNA synthesis. Preincubation with VAS2870 (10 and 20 μM) completely abolishes PDGF-mediated NADPH oxidase activation and ROS production. Preincubation with VAS2870 (0.1-20 μM) does not affect PDGF-induced cell cycle progression. However, it abolishes PDGF-dependent chemotaxis of VSMC in a concentration-dependent manner (100% inhibition at 10 μM)[1]. VAS2870 inhibits dose-dependently autocrine increase of cell number in FaO rat hepatoma cells, and almost completely blocked ROS production and thymidine incorporation when used at 25 mM. VAS2870 blocks serum-dependent cell growth of FaO rat hepatoma cells. VAS2870 inhibits proliferation of different human hepatocellular carcinoma (HCC) cell lines. VAS2870 pretreatment enhances TGF-b-mediated apoptosis of FaO rat hepatoma cells[2]. |
| Kinase Assay | 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 Assay | 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 |
| Density | 1.5±0.1 g/cm3 |
|---|---|
| Boiling Point | 627.0±65.0 °C at 760 mmHg |
| Molecular Formula | C18H12N6OS |
| Molecular Weight | 360.392 |
| Flash Point | 333.0±34.3 °C |
| Exact Mass | 360.079315 |
| LogP | 3.61 |
| Vapour Pressure | 0.0±1.8 mmHg at 25°C |
| Index of Refraction | 1.808 |
| Storage condition | 2-8℃ |
