VAS 3947

目录号: PL01910 纯度: ≥99%
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)。
CAS No. :869853-70-3
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中文名称
VAS 3947
英文名称
VAS 3947
英文别名
VAS3947;3-benzyl-7-(2-oxazolyl)thio-1,2,3-triazolo[4,5-d]pyrimidine;2-((3-benzyl-3H-[1,2,3]triazolo[4,5-d]pyrimidin-7-yl)thio)oxazole;2-(3-benzyltriazolo[4,5-d]pyrimidin-7-yl)sulfanyl-1,3-oxazole;VU0508924-1;VAS 3947
Cas No.
869853-70-3
分子式
C14H10N6Os
分子量
310.33
包装储存
Powder -20°C 3 years;4°C 2 years
详情描述
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)。
产品详情
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)。
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.
性状
Solid
体外研究(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
体内研究(In Vivo)
NADPH 氧化酶抑制剂 has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
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.
[3]. Lu WJ, et
溶解度数据
In Vitro: DMSO : 100 mg/mL (322.24 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)
[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

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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