| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| Targets |
NF-κB; COX-2; iNOS
Dehydroevodiamine targets multiple pathways and enzymes. It has antiarrhythmic effects through modulation of cardiac ion channels in ventricular myocytes. The compound inhibits LPS-induced expression of iNOS, COX-2, PGE2, and NF-κB, indicating anti-inflammatory activity through the inhibition of the NF-κB pathway and downstream inflammatory mediators. It also has anticholinesterase activity, which may contribute to its anti-amnesic effects. Its ability to improve beta-amyloid type amnesia suggests potential interactions with cholinergic and amyloid signaling pathways. The compound's hypotensive and negative chronotropic effects indicate modulation of cardiovascular function. |
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| ln Vitro |
The volume of distribution and clearance were shown to be independent of dose by the dose ranging study. The drug is primarily eliminated through metabolism[2]. Dehydroevodiamine was administered intravenously, which resulted in a noticeable decrease in heart rate and a small but significant drop in blood pressure[3].
In vitro studies have demonstrated that dehydroevodiamine has an antiarrhythmic effect on guinea pig ventricular myocytes. It inhibits LPS-induced expression of iNOS, COX-2, PGE2, and NF-κB in mouse macrophages, indicating potent anti-inflammatory activity. The compound has anticholinesterase activity. Its ability to improve beta-amyloid type amnesia suggests neuroprotective effects. The compound's hypotensive and negative chronotropic activities have been documented in various in vitro models. |
| ln Vivo |
Dehydroevodiamine was applied to the cells in vitro at different concentrations for 2 to 10 days (1–20 μM). The viable cells were counted ten days after plating.
In vivo, dehydroevodiamine has been shown to have hypotensive and negative chronotropic effects. Its antiarrhythmic effects have been demonstrated in animal models. The compound's anti-amnesic effects and ability to improve beta-amyloid type amnesia suggest potential therapeutic applications in neurodegenerative diseases. Its anti-inflammatory activity may contribute to its overall therapeutic benefits in vivo. However, comprehensive in vivo efficacy and safety studies are needed to fully evaluate its therapeutic potential. The compound's natural occurrence in Evodia rutaecarpa, which has a long history of use in traditional Chinese medicine, supports its potential as a lead compound for drug development. |
| Enzyme Assay |
In vitro non-cell enzyme/receptor binding assays for dehydroevodiamine typically involve measuring the inhibition of cholinesterase activity using purified enzyme and a chromogenic substrate such as acetylthiocholine. The compound is incubated with the enzyme and substrate, and the production of thiocholine is measured spectrophotometrically. The inhibition of iNOS and COX-2 activities can be measured using cell-free enzyme assays with purified enzymes and appropriate substrates. NF-κB binding to DNA can be assessed using EMSA or ELISA-based assays. These assays provide quantitative data on the compound's direct interactions with its molecular targets.
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| Cell Assay |
In vitro cell-based assays for dehydroevodiamine use various cell lines to study its biological activities. For anti-inflammatory studies, mouse macrophages stimulated with LPS are used, and the expression of iNOS, COX-2, PGE2, and NF-κB is measured by Western blotting, qPCR, or ELISA. For cardiac studies, ventricular myocytes are used to study the compound's effects on ion channel currents using patch-clamp electrophysiology. For neuroprotective studies, neuronal cell lines are used to study the compound's effects on amyloid pathology and cholinergic signaling. Cell viability is assessed using MTT or similar assays.
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| Animal Protocol |
Sprague-Dawley rats
1, 2.5, and 10 mg/kg intravenous infusion In vivo animal studies for dehydroevodiamine employ models of cardiac arrhythmia, inflammation, and neurodegeneration. For antiarrhythmic studies, animal models of arrhythmia induced by coronary artery ligation or pharmacological agents are used, and electrocardiographic parameters are monitored. For anti-inflammatory studies, models such as LPS-induced inflammation are used, and parameters such as inflammatory cytokine levels and immune cell infiltration are assessed. For neuroprotective studies, models of beta-amyloid-induced amnesia are used, and cognitive function is assessed using behavioral tests such as the Morris water maze. Pharmacokinetic studies in these models provide information about the compound's absorption, distribution, metabolism, and excretion. |
| ADME/Pharmacokinetics |
Dehydroevodiamine has a molecular weight of 301.34 g/mol and a molecular formula of C₁₉H₁₅N₃O. It is a quinazoline alkaloid isolated from Evodiae Fructus. The compound is also known by various synonyms and is commercially available as a high-purity research compound (≥98%). It should be stored under appropriate conditions as recommended by the manufacturer. Detailed pharmacokinetic parameters such as absorption, distribution, metabolism, and excretion have not been extensively characterized. As a small molecule alkaloid, dehydroevodiamine is expected to have moderate oral bioavailability and to cross the blood-brain barrier, consistent with its neuroprotective effects.
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| Toxicity/Toxicokinetics |
The toxicity profile of dehydroevodiamine has not been comprehensively evaluated in published studies. As a natural alkaloid from Evodia rutaecarpa, which has a history of use in traditional medicine, it is generally considered to have moderate toxicity. The compound's ability to inhibit ion channels and modulate cardiac function suggests that it may have significant cardiovascular effects that require careful evaluation. The compound is classified as a research reagent and is not intended for human therapeutic use without further safety evaluation. Standard laboratory safety precautions should be followed when handling the compound, including the use of appropriate personal protective equipment and working in a well-ventilated area.
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| References | |
| Additional Infomation |
Reports indicate that dehydroevorutin has been found in rutin (Tetradium ruticarpum), and relevant data are available for reference.
Dehydroevodiamine is a major bioactive quinazoline alkaloid isolated from the unripe fruit of Evodia rutaecarpa (Evodiae Fructus). It has a number of biological effects, including hypotensive, negative chronotropic, and ion channel depressant activities. The compound has an antiarrhythmic effect on guinea pig ventricular myocytes. It inhibits LPS-induced expression of iNOS, COX-2, PGE2, and NF-κB in mouse macrophages. Dehydroevodiamine also has anticholinesterase activity and an anti-amnesic effect, and it may be a novel and effective ligand for improvement of beta-amyloid type amnesia. Not approved for clinical use; intended for research purposes only. |
| Molecular Formula |
C19H15N3O
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| Molecular Weight |
301.3419
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| Exact Mass |
301.121
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| CAS # |
67909-49-3
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| Related CAS # |
Dehydroevodiamine hydrochloride;111664-82-5
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| PubChem CID |
9817839
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| Appearance |
Light yellow to yellow solid powder
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| Melting Point |
216-218ºC
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| LogP |
2.159
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
23
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| Complexity |
753
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
VXHNSVKJHXSKKM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H15N3O/c1-21-16-9-5-3-7-14(16)19(23)22-11-10-13-12-6-2-4-8-15(12)20-17(13)18(21)22/h2-9H,10-11H2,1H3
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| Chemical Name |
21-methyl-3,13,21-triazapentacyclo[11.8.0.02,10.04,9.015,20]henicosa-1,3,5,7,9,15,17,19-octaen-14-one
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| Synonyms |
Dehydroevodiamine
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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: ~8.3 mg/mL (~27.6 mM)
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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 | 3.3185 mL | 16.5926 mL | 33.1851 mL | |
| 5 mM | 0.6637 mL | 3.3185 mL | 6.6370 mL | |
| 10 mM | 0.3319 mL | 1.6593 mL | 3.3185 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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