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| 5mg |
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| 10mg |
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| Targets |
VAS 2870 targets NAD(P)H oxidase (Nox), a family of enzymes that generate superoxide and other reactive oxygen species. It is a pan-NADPH oxidase inhibitor and acts as a preferential NADPH Oxidase 2 (NOX2) inhibitor. It abolishes PDGF-mediated Nox activation and ROS production.
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| ln Vitro |
VAS2870 efficiently suppresses the generation of intracellular ROS and the PDGF-BB-dependent activation of NADPH oxidase. Moreover, VAS2870 blocks DNA synthesis but not PDGF-BB-dependent polymerization. The pre-carrier containing VAS2870 (10 and 20 μM) totally stopped the formation of ROS and NADPH oxidase activation caused by PDGF. Pre-vehicle VAS2870 (0.1–20 μM) has no effect on the advancement of the PDGF-mediated cell cycle. At 10 μM, it fully prevents the dose-dependent rise in cell number in FaO tray cells; yet, at 25 mM, it almost totally saturates the generation of ROS and causes thoracic stress. Disables FaO tray cells with VAS2870. Serum stimulates the development of cells. A variety of human hepatocellular carcinoma (HCC) cell lines are blocked by VAS2870. Pallet cells' TGF-b-mediated FaO is momentarily enhanced by VAS2870 [2].
In vitro, VAS 2870 inhibits PMA-induced oxidative burst in HL-60 cells with an IC50 of 2 μM. It inhibits oxidized-LDL-mediated, but not basal, ROS production in HUVECs. It also inhibits NOX activity in human cells with an IC50 of 10.6 μM. At 10 μM, it abolishes PDGF-mediated Nox activation and ROS production. |
| ln Vivo |
In vivo activity data for VAS 2870 are limited in the available literature. As a research compound, its primary application is in in vitro and cell-based studies of NOX function. Its ability to inhibit NOX-derived ROS production suggests potential for studying oxidative stress-related pathologies, but systematic in vivo efficacy studies are not extensively reported.
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| Enzyme Assay |
In vitro enzyme inhibition assays for VAS 2870 are performed using cell-free systems containing NADPH oxidase enzyme preparations. The enzyme activity is measured by detecting superoxide production using chemiluminescent or colorimetric probes. The compound is incubated with the enzyme and substrate (NADPH), and the inhibition of ROS production is quantified. IC50 values are calculated from concentration-response curves.
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| Cell Assay |
In vitro cellular assays for VAS 2870 are performed using cell lines such as HL-60 cells or HUVECs. Cells are stimulated with PMA or oxidized-LDL to induce oxidative burst, and ROS production is measured using fluorescent probes such as DCFH-DA or chemiluminescent assays. The compound's ability to inhibit ROS production is quantified, and IC50 values are calculated from concentration-response curves.
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| Animal Protocol |
In vivo animal experiments for VAS 2870 are not extensively documented. As a research compound, in vivo studies would typically involve administration to animal models of oxidative stress-related diseases. The compound would be administered via intraperitoneal or oral routes, and efficacy would be assessed by measuring oxidative stress markers, inflammation, and tissue damage.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of VAS 2870 have been characterized in part. The compound has a molecular weight of 360.4 g/mol and a purity of >98%. Its chemical name is 3-Benzyl-7-(2-benzoxazolyl)thio-1,2,3-triazolo(4,5-d)pyrimidine. It is soluble in DMSO. Further PK studies are needed to determine its absorption, distribution, metabolism, and excretion profile.
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| Toxicity/Toxicokinetics |
Toxicological data for VAS 2870 are not extensively reported. As a research-use compound, its safety profile has not been formally evaluated in comprehensive preclinical toxicology studies. The compound is intended for research purposes only and is not approved for human therapeutic use. Standard laboratory safety precautions should be followed when handling this compound.
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| References |
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| Additional Infomation |
VAS 2870 is a pan-NADPH oxidase inhibitor also known as NOX Inhibitor III. It inhibits PMA-induced oxidative burst in HL-60 cells with an IC50 of 2 μM. It is used in redox signaling research to study the role of NOX-derived reactive oxygen species in cytoskeletal organization, cell motility, and inflammation. This product is for research use only.
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| Molecular Formula |
C18H12N6OS
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|---|---|
| Molecular Weight |
360.392
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| Exact Mass |
360.079
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| CAS # |
722456-31-7
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| Related CAS # |
722456-31-7;
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| PubChem CID |
4058452
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
627.0±65.0 °C at 760 mmHg
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| Flash Point |
333.0±34.3 °C
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| Vapour Pressure |
0.0±1.8 mmHg at 25°C
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| Index of Refraction |
1.808
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| LogP |
3.61
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
26
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| Complexity |
479
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
HZSOKHVVANONPV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H12N6OS/c1-2-6-12(7-3-1)10-24-16-15(22-23-24)17(20-11-19-16)26-18-21-13-8-4-5-9-14(13)25-18/h1-9,11H,10H2
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| Chemical Name |
2-(3-benzyltriazolo[4,5-d]pyrimidin-7-yl)sulfanyl-1,3-benzoxazole
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~83.3 mg/mL (~231.14 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.94 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.94 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7748 mL | 13.8739 mL | 27.7477 mL | |
| 5 mM | 0.5550 mL | 2.7748 mL | 5.5495 mL | |
| 10 mM | 0.2775 mL | 1.3874 mL | 2.7748 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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