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^[1][2].

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^[1].
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^[2].
VAS3947 decreases ROS levels. VAS3947 triggers endoplasmic reticulum (ER) stress and consequent unfolding protein response (UPR)^[2].
VAS3947 attenuates platelet activation and thrombus formation via a NOX-independent pathway downstream of PKC^3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

NADPH 氧化酶抑制剂

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

310.33

C₁₄H₁₀N₆OS

869853-70-3

Room temperature in continental US; may vary elsewhere.

DMSO : 100 mg/mL (322.24 mM; Need ultrasonic)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2.5 mg/mL (8.06 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (8.06 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 2.

  请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

  Solubility: ≥ 2.5 mg/mL (8.06 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (8.06 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 3.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 2.5 mg/mL (8.06 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (8.06 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [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 al. VAS2870 and VAS3947 attenuate platelet activation and thrombus formation via a NOX-independent pathway downstream of PKC. Sci Rep. 2019;9(1):18852. Published 2019 Dec 11.