| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| Other Sizes |
| Targets |
Evocarpine targets voltage-dependent calcium channels, inhibiting Ca2+ influx. It also has antimycobacterial activity against mycobacteria including multidrug-resistant clinical isolates of Mycobacterium tuberculosis. The compound affects apoptosis and cAMP pathways. Its antibacterial effects are mediated through its interaction with calcium channels and possibly other cellular targets.
|
|---|---|
| ln Vitro |
Evocarpine (1-100 μM) applied cumulatively suppresses the sustained induced contraction by 60 mM K+ in a concentration-dependent manner [1]. In promyelocytic leukemia HL-60 cells, evocarpine has been shown to cause apoptotic cell death in time- and dose-dependent ways[3].
In vitro, evocarpine shows antimycobacterial activity and vasorelaxant effects. It inhibits Ca2+ influx through voltage-dependent calcium channels. Evocarpine induces apoptotic cell death in promyelocytic leukemia HL-60 cells. It exhibits antibacterial activity against various bacterial strains. The compound's activity against multidrug-resistant clinical isolates of Mycobacterium tuberculosis has been reported. |
| ln Vivo |
In vivo, evocarpine has vasorelaxant effects, suggesting potential cardiovascular applications. Its antimycobacterial activity has been evaluated in animal models of tuberculosis, although detailed in vivo studies are limited. The compound's ability to inhibit Ca2+ influx through voltage-dependent calcium channels may contribute to its vasorelaxant effects in vivo. Further studies are needed to fully characterize its in vivo pharmacokinetics and pharmacodynamics.
|
| Enzyme Assay |
For non-cellular assays, evocarpine is evaluated for its ability to inhibit Ca2+ influx through voltage-dependent calcium channels using patch-clamp techniques or fluorescence-based calcium flux assays in cell-free membrane preparations. Antimycobacterial activity is assessed using standard broth microdilution methods against Mycobacterium tuberculosis strains. Binding affinity to calcium channels can be assessed using radioligand binding assays.
|
| Cell Assay |
In vitro cell culture experiments are performed using various cell lines including HL-60 leukemia cells, mycobacterial cultures, and vascular smooth muscle cells. Cells are treated with evocarpine at concentrations ranging from 1 to 100 μM for 24-72 hours. Endpoints include cell viability (MTT assay), apoptosis (Annexin V/PI staining), calcium flux (Fluo-4 or Fura-2 imaging), and antibacterial activity (MIC determination). Antimycobacterial activity is assessed in infected macrophage cultures.
|
| Animal Protocol |
In vivo animal studies have been limited. Evocarpine is typically administered orally or intraperitoneally in rodent models. Vasorelaxant effects are assessed in vivo by measuring blood pressure or vascular reactivity. Antimycobacterial efficacy is evaluated in tuberculosis models by measuring bacterial load in tissues (lungs, spleen) and survival rates. Cardiovascular parameters such as heart rate and blood pressure are monitored.
|
| ADME/Pharmacokinetics |
Evocarpine has a molecular formula of C23H33NO and a molecular weight of approximately 339.5 g/mol. It is a quinolone alkaloid with moderate solubility in DMSO (≥52.1 mg/mL) and ethanol (≥50.6 mg/mL), but is insoluble in water. The compound is typically stored at -20°C under inert conditions. Pharmacokinetic properties are not well characterized, but the compound is expected to have moderate oral bioavailability due to its lipophilic nature.
|
| Toxicity/Toxicokinetics |
Evocarpine is considered a natural product with moderate toxicity. In vitro cytotoxicity has been observed in mammalian cell lines at higher concentrations. Antimycobacterial agent-4, a related compound, exhibits cytotoxicity on mammalian cell lines with an IC50 of 2.2 μM. Standard laboratory safety precautions should be followed when handling evocarpine. The compound is for research use only and is not intended for therapeutic applications.
|
| References |
|
| Additional Infomation |
Ivoricapin belongs to the quinoline class of compounds. It has been reported that iveric acid exists in the Rutaceae plant Tetradium ruticarpum, and relevant data are available for reference.
Evocarpine is a quinolone alkaloid isolated from Evodiae fructus, a traditional Chinese medicinal herb. It has antimycobacterial, vasorelaxant, and antibacterial activities. The compound inhibits Ca2+ influx through voltage-dependent calcium channels and induces apoptosis in HL-60 leukemia cells. It is used in research on anti-infective agents, cardiovascular pharmacology, and natural product chemistry. It is for research use only and is not approved for clinical use. |
| Molecular Formula |
C23H33NO
|
|---|---|
| Molecular Weight |
339.51
|
| Exact Mass |
339.256
|
| CAS # |
15266-38-3
|
| PubChem CID |
5317303
|
| Appearance |
White to off-white solid powder
|
| Density |
1.0±0.1 g/cm3
|
| Boiling Point |
456.2±45.0 °C at 760 mmHg
|
| Melting Point |
34-38℃
|
| Flash Point |
156.1±18.1 °C
|
| Vapour Pressure |
0.0±1.1 mmHg at 25°C
|
| Index of Refraction |
1.526
|
| LogP |
7.7
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
11
|
| Heavy Atom Count |
25
|
| Complexity |
451
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CCCC/C=C\CCCCCCCC1=CC(=O)C2=CC=CC=C2N1C
|
| InChi Key |
HWFYWIVOYBPLQU-SREVYHEPSA-N
|
| InChi Code |
InChI=1S/C23H33NO/c1-3-4-5-6-7-8-9-10-11-12-13-16-20-19-23(25)21-17-14-15-18-22(21)24(20)2/h6-7,14-15,17-19H,3-5,8-13,16H2,1-2H3/b7-6-
|
| Chemical Name |
1-methyl-2-[(Z)-tridec-8-enyl]quinolin-4-one
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : 100 mg/mL (294.54 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.36 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 (7.36 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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 (7.36 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 | 2.9454 mL | 14.7271 mL | 29.4542 mL | |
| 5 mM | 0.5891 mL | 2.9454 mL | 5.8908 mL | |
| 10 mM | 0.2945 mL | 1.4727 mL | 2.9454 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
