产品
编 号:F489021
分子式:C14H10N6OS
分子量:310.33
产品类型
结构图
CAS No: 869853-70-3
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产品详情
生物活性:
VAS 3947, a specific NADPH oxidase (NOX) inhibitor, exerts a potent antiplatelet effect. VAS3947 induces apoptosis independently of anti-NOX activity, via UPR activation, mainly due to aggregation and misfolding of proteins.
体内研究:
NADPH 氧化酶抑制剂
体外研究:
VAS3947 consistently inhibits NADPH oxidase activity in low micromolar concentrations, and interferes neither with ROS detection nor with XOD or eNOS activities. VAS3947 (30 μM) does not interfere with xanthine/XOD-derived L012 signals, suggesting this compound is free of antioxidant or scavenging effects relevant to ROS detection. In CaCo-2 cell homogenates, VAS3947 completely blocks NADPH-dependent ROS production with an IC50 of 12 μM.VAS3947 triggers cell proliferation arrest and death independently of anti-NOX activity. The IC50 values of the different cell lines ranges from 2.6 ± 0.6 μM for the most sensitive cell line MV-4-11 to 4.9 μM for THP-1, the least sensitive.VAS3947 decreases ROS levels. VAS3947 triggers endoplasmic reticulum (ER) stress and consequent unfolding protein response (UPR).VAS3947 attenuates platelet activation and thrombus formation via a NOX-independent pathway downstream of PKC3].