| Size | Price | Stock | Qty |
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| 100mg |
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| 500mg |
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| 1g |
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| Other Sizes |
| Targets |
The mechanism of action of Emoxypine involves multiple molecular targets. It primarily functions as an antioxidant, directly scavenging free radicals and inhibiting lipid peroxidation. Studies show that Emoxypine modulates monoamine oxidase activity: in vitro, it reduces MAO-A activity by 34-44% and MAO-B activity by 9-10%. The compound also exhibits iron-chelating properties by binding free iron ions. Furthermore, Emoxypine has membrane-protective effects, reducing cell membrane viscosity and enhancing binding interactions at the GABA-benzodiazepine receptor complex. As an anxiolytic agent, it exerts effects through GABA-modulating action and demonstrates activity in inhibiting ion currents via the NMDA receptor complex.
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| ln Vitro |
In vitro studies demonstrate that Emoxypine exhibits multiple biological activities. In enzyme activity assays, Emoxypine reduces MAO-A activity by 34-44% (p < 0.05) and MAO-B activity by 9-10% (p < 0.05) within the pharmacokinetic concentration range (10⁻⁹ to 10⁻⁶ M). Studies show that Emoxypine possesses iron-chelating properties, binding free iron ions, which provides a basis for its potential application in neurodegenerative conditions such as Alzheimer's disease as well as hematologic disorders like thalassemia and hemochromatosis. Furthermore, in rabbit granulocyte experiments, 5 mM Emoxypine virtually precluded lipopolysaccharide-induced granulocyte aggregation and completely abolished LPS-induced thromboxane B2 and prostaglandin F2α production.
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| ln Vivo |
In vivo studies demonstrate that Emoxypine exhibits significant activity in various animal models. In a skin ischemia model using male albino rats, administration of Mexidol at 25 mg/kg for 3 days decreased aspartate transaminase and creatine phosphokinase activity and arrested the progression of skin necrosis. Studies show that Emoxypine increases catalase and glutathione peroxidase activity, neutralizing hydrogen peroxide radicals. Furthermore, Emoxypine counteracts ATP loss in cerebral and myocardial ischemia and maintains oxidative phosphorylation by increasing succinate dehydrogenase activity. In modulating central nervous system function, Emoxypine inhibits ion currents via the NMDA receptor complex and enhances binding at the GABA-benzodiazepine receptor complex.
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| Enzyme Assay |
In vitro enzyme activity studies of Emoxypine primarily focus on its modulation of monoamine oxidase. A typical protocol includes: 1) Prepare mitochondrial fractions from rat liver as a source of MAO enzyme; 2) Dissolve Emoxypine in appropriate buffer to prepare serial concentrations (10⁻⁹ to 10⁻⁶ M); 3) Pre-incubate the drug with the enzyme preparation for 10 minutes at 37°C; 4) Add specific substrates: serotonin for MAO-A or phenylethylamine for MAO-B; 5) Incubate for 30-60 minutes at 37°C; 6) Detect reaction product formation (e.g., aldehydes) using fluorometric or spectrophotometric methods; 7) Calculate the percentage inhibition of MAO-A and MAO-B activity to evaluate the modulatory effect of the drug.
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| Cell Assay |
The in vitro cell assay protocol for Emoxypine is as follows: 1) Isolate target cells (e.g., rabbit venous blood granulocytes, neuronal cells, or hepatocytes); 2) Resuspend cells in appropriate medium and place in aggregometer cuvettes; 3) Add Emoxypine (e.g., 5 mM) or its solvent and incubate for 2 minutes at 37°C; 4) Add stimulant (e.g., lipopolysaccharide 200 μg/mL) to induce cell activation; 5) Trace aggregation response for 5 minutes; 6) Collect supernatants and measure eicosanoid production including thromboxane B2, prostaglandin E, and prostaglandin F2α using radioimmunoassay methods; 7) Assess cell viability using MTT or trypan blue staining.
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| Animal Protocol |
An in vivo animal assay protocol for Emoxypine using a skin ischemia model as an example: 1) Use male albino rats; 2) Establish a skin ischemia model; 3) Randomize animals into model control, vehicle control, and Emoxypine treatment groups (25 mg/kg, for 3 days); 4) Administration routes include intraperitoneal injection, intramuscular injection, or oral gavage; 5) Following treatment, measure biochemical parameters: assess aspartate transaminase and creatine phosphokinase activity to evaluate the extent of cytolysis; 6) Measure antioxidant enzyme activity: determine catalase and glutathione peroxidase levels; 7) Perform histopathological examination to assess necrotic area and inflammatory infiltration. Additionally, in seizure models, PTZ-induced seizure can be used to evaluate the inhibitory effects of Emoxypine on ROS and NO formation.
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| ADME/Pharmacokinetics |
Pharmacokinetic studies of Emoxypine demonstrate its favorable ability to penetrate the blood-brain barrier, attributed to its low molecular weight (137.18 Da) and appropriate physicochemical properties. Due to its hydrophilic nature, Emoxypine itself has limited transport capacity to nervous tissues and brain, leading to the development of derivatives with increased lipophilicity (such as the succinate salt) to enhance BBB permeability. Emoxypine and its metabolites can be detected in human urine, with excretion profiles correlated to the route of administration. It is primarily metabolized in the liver, with metabolites excreted via the kidneys.
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| Toxicity/Toxicokinetics |
Based on available research data, Emoxypine demonstrates a favorable safety profile. In the MeSH database, Emoxypine is classified as a compound with various pharmacological effects including antiarrhythmic, antioxidant, antiplatelet, psychotropic, and radioprotective activities, but it is also listed as a mutagen. In animal studies, no significant toxicity has been observed at conventional therapeutic doses. As a pharmaceutical ingredient that has been used clinically in Russia for many years, the safety of Emoxypine in humans has been clinically validated. In toxicological classifications, the compound has a hazard code of Xi (irritant). It is worth noting that Emoxypine has not yet received FDA approval for marketing and is primarily used for scientific research purposes in the United States.
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| References |
[1]. https://pubchem.ncbi.nlm.nih.gov/compound/114681
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| Additional Infomation |
Emoxypine is being investigated in the clinical trial NCT06221826 (MEXIDOL® for the rehabilitation of patients with acute brain failure). The second source of the compound is hydrogen chloride; it has been used as a retinal protectant.
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| Molecular Formula |
C8H11NO
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| Molecular Weight |
137.18
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| Exact Mass |
137.084
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| CAS # |
2364-75-2
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| Related CAS # |
127464-43-1
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| PubChem CID |
114681
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
280.6±35.0 °C at 760 mmHg
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| Melting Point |
136-138ºC
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| Flash Point |
123.5±25.9 °C
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| Vapour Pressure |
0.0±0.6 mmHg at 25°C
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| Index of Refraction |
1.536
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| LogP |
2.09
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
10
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| Complexity |
105
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(C1C(O)=CC=C(C)N=1)C
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| InChi Key |
JPGDYIGSCHWQCC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C8H11NO/c1-3-7-8(10)5-4-6(2)9-7/h4-5,10H,3H2,1-2H3
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| Chemical Name |
2-ethyl-6-methylpyridin-3-ol
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| Synonyms |
emoxypin; 6-Methyl-2-ethyl-3-hydroxypyridine; 2-Ethyl-6-methyl-3-oxypyridine; RefChem:590760; ...; Emoxypine;
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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 | 7.2897 mL | 36.4485 mL | 72.8969 mL | |
| 5 mM | 1.4579 mL | 7.2897 mL | 14.5794 mL | |
| 10 mM | 0.7290 mL | 3.6448 mL | 7.2897 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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