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)。

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.

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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

NADPH 氧化酶抑制剂 has not independently confirmed the accuracy of these methods. They are for reference only.

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[1]. Wind S, et al. Comparative pharmacology of chemically distinct NADPH oxidase inhibitors. Br J Pharmacol. 2010;161(4):885-898.
[2]. El Dor M, et al. VAS3947 Induces UPR-Mediated Apoptosis through Cysteine Thiol Alkylation in AML Cell Lines. Int J Mol Sci. 2020;21(15):5470. Published 2020 Jul 31.
[3]. Lu WJ, et

In Vitro: DMSO : 100 mg/mL (322.24 mM; Need ultrasonic)配制储备液