[CAS NO. 869853-70-3] VAS 3947
PRODUCTS SPECIFICATIONS [869853-70-3]
DESCRIPTION [869853-70-3]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 310.33 |
| Molecular Formula | C14H10N6OS |
| SMILES | C12=NC=NC(SC3=NC=CO3)=C1N=NN2CC4=CC=CC=C4 |
Summary
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] .
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 IC
50
of 12 µM
[1]
.
VAS3947 triggers cell proliferation arrest and death independently of anti-NOX activity. The IC
50
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
NADPH 氧化酶抑制剂
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 100 mg/mL ( 322.24 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.2224 mL | 16.1119 mL | 32.2238 mL |
| 5 mM | 0.6445 mL | 3.2224 mL | 6.4448 mL |
| 10 mM | 0.3222 mL | 1.6112 mL | 3.2224 mL |
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.