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VAS 3947

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Chemical Structure| 869853-70-3 同义名 : -
CAS号 : 869853-70-3
货号 : A1554653
分子式 : C14H10N6OS
纯度 : 98%
分子量 : 310.334
MDL号 : -
存储条件:

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(338.35 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
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
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

[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.