| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Nox-2/4[1]
NADPH oxidase 2 (NOX2) and NADPH oxidase 4 (NOX4). GLX481304 is a specific and potent dual inhibitor of these two NOX isoforms, with an IC50 of approximately 1.25 microM for both. It is a cell-permeable, non-cytotoxic inhibitor with good selectivity over NOX1. |
|---|---|
| ln Vitro |
GLX481304 is a specific inhibitor of NOX2 and NOX4 with an IC50 of 1.25 microM for both isoforms. It effectively suppresses reactive oxygen species (ROS) production in isolated mouse cardiomyocytes and improves their contractility. The compound has no general antioxidant effects and does not inhibit NOX1, making it a specific tool for studying NOX2/4 function.
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| ln Vivo |
In vivo, GLX481304 improves cardiomyocyte contractility in isolated mouse hearts, particularly after an ischemia-reperfusion challenge, by inhibiting ROS production. This suggests that the compound can protect the heart from oxidative stress-induced damage and improve functional recovery after an ischemic event. These findings make GLX481304 a promising compound for research into ischemic heart injury.
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| Enzyme Assay |
For non-cellular assays, the activity of NOX2 and NOX4 can be measured in cell-free systems using recombinant enzymes or membrane fractions containing the oxidase. GLX481304 is added at varying concentrations (0.1-50 microM). The production of superoxide is measured by the reduction of cytochrome c or by a luminescence-based method (e.g., lucigenin chemiluminescence). IC50 values for each isoform are calculated from the resulting dose-response curves.
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| Cell Assay |
For cell-based assays, primary mouse cardiomyocytes are isolated and incubated with GLX481304 (0.5-10 microM) for 30-60 minutes. ROS production is then stimulated by hypoxia-reoxygenation (or by an agent like PMA) and measured using a fluorescent probe such as DCFH-DA or DHE. Cell contractility is assessed using a video-based edge-detection system or by measuring calcium transients. The compound's effect on both ROS levels and contractile function is assessed simultaneously.
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| Animal Protocol |
For animal studies, GLX481304 can be delivered to the heart by intraperitoneal injection (IP) or by intravenous (IV) administration to mice prior to an ischemia-reperfusion procedure. Doses would need to be optimized. In the isolated perfused heart model (Langendorff), the compound can be added directly to the perfusate. The primary endpoints are the recovery of left ventricular developed pressure (LVDP) and the reduction of infarct size (determined by TTC staining). ROS production in the heart is measured in tissue homogenates.
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| ADME/Pharmacokinetics |
GLX481304 is a small molecule with a molecular formula of C13H15N9 and a molecular weight of 297.32 g/mol. It is cell-permeable, soluble in DMSO, and has good stability. The compound is non-cytotoxic, which is a valuable property for a potential therapeutic or research tool. The powder is stored at -20degC for long-term stability.
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| Toxicity/Toxicokinetics |
GLX481304 is described as non-cytotoxic in the literature, indicating that it does not cause cell death at concentrations that are effective for NOX2/4 inhibition. Material safety data sheets indicate that it may be harmful if swallowed and may be very toxic to aquatic life. Standard laboratory safety precautions, including the use of gloves and eye protection, should be followed.
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| References | |
| Additional Infomation |
GLX481304 was identified through a chemical library screening and was first reported in a 2021 Scientific Reports publication. The compound is a valuable tool for dissecting the distinct roles of NOX2 and NOX4 in cardiovascular diseases, as well as in neurodegenerative diseases and other conditions involving oxidative stress. It is not an approved drug and is intended for research use only.
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| Molecular Formula |
C23H29N7O
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|---|---|
| Molecular Weight |
419.522663831711
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| Exact Mass |
419.243
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| CAS # |
701224-63-7
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| PubChem CID |
1214345
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| Appearance |
White to off-white solid powder
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| LogP |
3.7
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
31
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| Complexity |
544
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=C(C=C(C=C1)NC2=NC(=NC(=N2)N)CN3CCN(CC3)C4=CC(=CC=C4)OC)C
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| InChi Key |
STKSULQULJWEMU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H29N7O/c1-16-7-8-18(13-17(16)2)25-23-27-21(26-22(24)28-23)15-29-9-11-30(12-10-29)19-5-4-6-20(14-19)31-3/h4-8,13-14H,9-12,15H2,1-3H3,(H3,24,25,26,27,28)
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| Chemical Name |
2-N-(3,4-dimethylphenyl)-6-[[4-(3-methoxyphenyl)piperazin-1-yl]methyl]-1,3,5-triazine-2,4-diamine
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3837 mL | 11.9184 mL | 23.8368 mL | |
| 5 mM | 0.4767 mL | 2.3837 mL | 4.7674 mL | |
| 10 mM | 0.2384 mL | 1.1918 mL | 2.3837 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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