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869853-70-3

869853-70-3 structure
869853-70-3 structure
  • Name: VAS 3947
  • Chemical Name: 3-Benzyl-7-(1,3-oxazol-2-ylsulfanyl)-3H-[1,2,3]triazolo[4,5-d]pyrimidine
  • CAS Number: 869853-70-3
  • Molecular Formula: C14H10N6OS
  • Molecular Weight: 310.334
  • Catalog: Signaling Pathways Apoptosis Apoptosis
  • Create Date: 2021-09-12 17:33:16
  • Modify Date: 2024-01-12 07:59:50
  • 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].

Name 3-Benzyl-7-(1,3-oxazol-2-ylsulfanyl)-3H-[1,2,3]triazolo[4,5-d]pyrimidine
Synonyms 3-Benzyl-7-(1,3-oxazol-2-ylsulfanyl)-3H-[1,2,3]triazolo[4,5-d]pyrimidine
3H-1,2,3-Triazolo[4,5-d]pyrimidine, 7-(2-oxazolylthio)-3-(phenylmethyl)-
Description 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].
Related Catalog
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[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 PKC3].
In Vivo NADPH 氧化酶抑制剂
References

[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.

Density 1.6±0.1 g/cm3
Boiling Point 577.8±60.0 °C at 760 mmHg
Molecular Formula C14H10N6OS
Molecular Weight 310.334
Flash Point 303.3±32.9 °C
Exact Mass 310.063690
LogP 1.96
Vapour Pressure 0.0±1.5 mmHg at 25°C
Index of Refraction 1.801
Storage condition 2-8°C
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