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| 5mg |
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| 10mg |
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| Targets |
The primary target of Evolitrine is cyclooxygenase (COX) enzymes, which it inhibits. COX enzymes are key mediators of the inflammatory response through the production of prostaglandins. By inhibiting COX, Evolitrine reduces inflammation and pain. The compound also has antifeedant activity, suggesting it may target insect feeding receptors or pathways. These targets make it relevant for anti-inflammatory and pest control research.
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| ln Vitro |
In vitro, Evolitrine demonstrates anti-inflammatory activity by inhibiting COX enzymes and reducing prostaglandin biosynthesis. The compound is isolated from Acronychia pedunculata and shows significant anti-inflammatory effects in cell-based assays. It also exhibits antifeedant activity in insect models. These in vitro activities support its use in research on inflammation, pain, and natural product-based pest control. The compound's detergent properties may affect its cellular interactions.
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| ln Vivo |
In vivo, Evolitrine has demonstrated anti-inflammatory activity in animal models. Its inhibition of COX enzymes suggests potential applications in treating inflammatory conditions. However, detailed in vivo efficacy data are limited. The compound is a natural alkaloid from plants used in traditional medicine. Further studies are needed to fully characterize its therapeutic potential, pharmacokinetics, and safety profile in animal models of inflammation and pain.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for Evolitrine include COX-1 and COX-2 inhibition assays using purified enzymes and appropriate substrates. The compound is incubated with COX enzymes at concentrations ranging from 0.1-100 μM, and enzyme activity is measured by prostaglandin production using ELISA or radiometric assays. IC50 values are determined by plotting percent inhibition versus inhibitor concentration. The compound's antifeedant activity is assessed in insect feeding assays. All assays include appropriate controls and reference compounds (e.g., indomethacin for COX inhibition).
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| Cell Assay |
In vitro cell-based assays for Evolitrine are conducted using inflammatory cell models (e.g., macrophages or monocytes) to assess anti-inflammatory activity. Cells are treated with Evolitrine at concentrations ranging from 0.1-100 μM, followed by stimulation with LPS or other inflammatory inducers. Pro-inflammatory cytokine levels (e.g., TNF-α, IL-6) and prostaglandin E2 are measured by ELISA. Cell viability is assessed using MTT assays. The compound's effects on COX expression and activity are evaluated by Western blot or activity assays. Experiments include vehicle controls and positive controls (e.g., NSAIDs).
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| Animal Protocol |
In vivo animal studies with Evolitrine are limited, as the compound is primarily used as a research tool. Anti-inflammatory studies may be conducted in rodent models of acute inflammation (e.g., carrageenan-induced paw edema or formalin-induced pain). The compound is administered via intraperitoneal or oral administration at doses ranging from 1-50 mg/kg. Inflammation is assessed by measuring paw edema, pain responses, or inflammatory markers. Each group consists of 6-10 animals with vehicle-treated and positive control groups. Further studies are needed for comprehensive characterization.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Evolitrine have not been extensively characterized. As a lipophilic furoquinoline alkaloid (MW 229.23), it is expected to have good oral bioavailability and tissue distribution, including penetration of the blood-brain barrier. The compound's detergent properties may affect its absorption and distribution. Metabolism likely occurs through hepatic cytochrome P450 enzymes, with elimination via biliary and renal excretion. Detailed PK parameters such as half-life, Cmax, and AUC require further investigation.
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| Toxicity/Toxicokinetics |
Toxicological data for Evolitrine are limited, as the compound is a natural product research tool. No significant toxicity has been reported at concentrations used for in vitro studies. The compound is an alkaloid from plants used in traditional medicine, suggesting a reasonable safety profile. However, comprehensive toxicological studies have not been conducted. As with all research chemicals, appropriate safety precautions should be taken during handling, and the compound should be used only for research purposes.
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| References | |
| Additional Infomation |
Evolitrine has reportedly been found in Melicope triphylla, Melicope semecarpifolia, and other organisms with available data.
Evolitrine is a furoquinoline alkaloid with significant anti-inflammatory activity through COX enzyme inhibition. It is isolated from Acronychia pedunculata and other plants. The compound also exhibits antifeedant activity. It is known as 7-methoxydictamnine and has a detergent-like property that dissolves fats for absorption. Evolitrine is used in research on inflammation, pain, and natural product pharmacology. Not approved for clinical therapeutic use; intended for research purposes only. |
| Molecular Formula |
C13H11NO3
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|---|---|
| Molecular Weight |
229.23134
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| Exact Mass |
229.074
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| CAS # |
523-66-0
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| PubChem CID |
196980
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.261g/cm3
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| Boiling Point |
381ºC at 760mmHg
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| Melting Point |
115℃
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| Flash Point |
184.2ºC
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| Index of Refraction |
1.642
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| LogP |
2.998
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
17
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| Complexity |
273
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
TWGHMXOYRUTQOL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H11NO3/c1-15-8-3-4-9-11(7-8)14-13-10(5-6-17-13)12(9)16-2/h3-7H,1-2H3
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| Chemical Name |
4,7-dimethoxyfuro[2,3-b]quinoline
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~100 mg/mL (~436.24 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.91 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 (10.91 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (10.91 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.3624 mL | 21.8122 mL | 43.6243 mL | |
| 5 mM | 0.8725 mL | 4.3624 mL | 8.7249 mL | |
| 10 mM | 0.4362 mL | 2.1812 mL | 4.3624 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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