生物活性 | |||
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描述 | VAS 3947 is a specific NOX inhibitor with potent antiplatelet effects. VAS3947 induces apoptosis through UPR activation, independent of anti-NOX activity[1][2].VAS3947 consistently inhibits NADPH oxidase activity at low micromolar concentrations and does not interfere with either the ROS assay or XOD or eNOS activity. VAS3947 (30 µM) does not interfere with xanthine/XOD-derived L012 signalling, suggesting that the compound does not have antioxidant or scavenging effects associated with the ROS assay. In CaCo-2 cell homogenates, VAS3947 completely blocked NADPH-dependent ROS production with an IC50 of 12 µM[1].Cell proliferation arrest and death induced by VAS 3947 were not associated with anti-NOX activity. IC50 values for different cell lines ranged from 2.6 ± 0.6 µM for the most sensitive cell line, MV-4-11, to 4.9 µM for the least sensitive cell line, THP-1. VAS 3947 reduces the level of ROS, triggering endoplasmic reticulum stress and the ensuing folding protein response (UPR)[2]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.22mL 0.64mL 0.32mL |
16.11mL 3.22mL 1.61mL |
32.22mL 6.44mL 3.22mL |
参考文献 |
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