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VAS 3947

CAS No. : 869853-70-3

MCE 国际站：VAS 3947

产品活性：VAS 3947 是一种特异的 NADPH 氧化酶 (NOX) 抑制剂，具有强大的抗血小板作用。VAS 3947 通过 UPR 激活，主要由于蛋白质聚集和错误折叠，独立于抗 NOX 活性诱导细胞凋亡 (apoptosis)。

研究领域：Metabolic Enzyme/Protease  |  Apoptosis

作用靶点：NADPH Oxidase  |  Apoptosis

In Vitro: 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 PKC^3].

In Vivo: NADPH 氧化酶抑制剂

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货号: HY-111447

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