| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Targets |
Lycoramine targets acetylcholinesterase (AChE), the enzyme responsible for the hydrolysis of acetylcholine. By inhibiting AChE, lycoramine increases the levels of acetylcholine in the synaptic cleft, enhancing cholinergic neurotransmission. This mechanism is similar to that of galantamine, which is used for the symptomatic treatment of Alzheimer's disease. Lycoramine may also have additional targets, such as nicotinic acetylcholine receptors, contributing to its neuroprotective effects.
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| ln Vitro |
In vitro, lycoramine exhibits acetylcholinesterase inhibitory activity, although it is generally less potent than galantamine. It has been shown to inhibit AChE in a concentration-dependent manner. Additionally, lycoramine may possess antioxidant and anti-inflammatory properties, contributing to its neuroprotective effects. These in vitro activities suggest its potential for the treatment of neurodegenerative diseases characterized by cholinergic deficits.
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| ln Vivo |
In vivo, lycoramine has demonstrated neuroprotective effects in animal models of cognitive impairment. It has been shown to improve learning and memory in rodent models of Alzheimer's disease. These effects are attributed to its AChE inhibitory activity and its ability to modulate cholinergic signaling. However, specific details of in vivo studies, such as the animal models used and the dosing regimens, are not extensively detailed in the available literature.
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| Enzyme Assay |
The in vitro enzyme assay for lycoramine typically measures its ability to inhibit acetylcholinesterase activity. These cell-free assays use purified AChE from electric eel or other sources and a chromogenic substrate such as acetylthiocholine. The compound's inhibitory potency (IC50) is determined by measuring the reduction in enzyme activity. These assays provide a direct measure of the compound's AChE inhibitory activity without the confounding effects of cellular uptake or metabolism.
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| Cell Assay |
In vitro cellular assays for lycoramine assess its neuroprotective effects in neuronal cell lines. Cells are treated with lycoramine and then exposed to a toxic insult, such as oxidative stress or β-amyloid peptide. Cell viability is measured using assays such as MTT. Additionally, the compound's effects on AChE activity in cells can be measured. These assays demonstrate the compound's ability to protect neurons from damage and inhibit AChE in a cellular context.
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| Animal Protocol |
In vivo animal studies for lycoramine have been conducted in rodent models of Alzheimer's disease or cognitive impairment. These models may involve administration of scopolamine to induce cholinergic deficits or the use of transgenic mouse models of Alzheimer's disease. Lycoramine is typically administered orally or intraperitoneally, and cognitive function is assessed using behavioral tests such as the Morris water maze. These studies demonstrate the compound's in vivo efficacy in improving cognitive function.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic data for lycoramine free base are not extensively detailed in the available literature. As a natural alkaloid, its pharmacokinetic properties would be similar to those of other Amaryllidaceae alkaloids. The compound's ability to cross the blood-brain barrier is important for its central nervous system activity. However, specific parameters such as half-life and bioavailability are not provided.
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| Toxicity/Toxicokinetics |
Specific toxicity data for lycoramine free base are not extensively detailed in the available literature. As an AChE inhibitor, its toxicity profile is likely related to its mechanism of action, potentially causing cholinergic side effects such as nausea, vomiting, and bradycardia at high doses. However, comprehensive toxicological studies are limited. The compound is intended for research use only and is not intended for human use.
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| References | |
| Additional Infomation |
Lycorine is a benzo[a]azapyridine compound. It has been reported to be found in Spirogyra, sea lettuce, and other organisms with relevant data.
Lycoramine free base is a research compound that is a natural alkaloid with acetylcholinesterase inhibitory and neuroprotective activities. It is structurally related to galantamine, an approved drug for Alzheimer's disease. Lycoramine is used as a tool for studying cholinergic signaling and neurodegenerative diseases. It is not approved for clinical use and is intended for research purposes only. |
| Molecular Formula |
C17H23NO3
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|---|---|
| Molecular Weight |
289.36942
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| Exact Mass |
289.168
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| CAS # |
21133-52-8
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| Related CAS # |
Lycoramine hydrobromide;89505-76-0
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| PubChem CID |
443723
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| Appearance |
White to off-white solid powder
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| Density |
1.25
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| Boiling Point |
436.4ºC at 760mmHg
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| Melting Point |
122-124ºC
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| Flash Point |
217.7ºC
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| Vapour Pressure |
2.17E-08mmHg at 25°C
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| Index of Refraction |
1.614
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| LogP |
2.012
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
21
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| Complexity |
404
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| Defined Atom Stereocenter Count |
3
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| SMILES |
CN1CC[C@@]23CC[C@@H](C[C@@H]2OC4=C(C=CC(=C34)C1)OC)O
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| InChi Key |
GJRMHIXYLGOZSE-JDFRZJQESA-N
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| InChi Code |
InChI=1S/C17H23NO3/c1-18-8-7-17-6-5-12(19)9-14(17)21-16-13(20-2)4-3-11(10-18)15(16)17/h3-4,12,14,19H,5-10H2,1-2H3/t12-,14-,17-/m0/s1
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| Chemical Name |
(1R,12S,14S)-9-methoxy-4-methyl-11-oxa-4-azatetracyclo[8.6.1.01,12.06,17]heptadeca-6(17),7,9-trien-14-ol
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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: 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)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~345.58 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.64 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 (8.64 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 (8.64 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 | 3.4558 mL | 17.2789 mL | 34.5578 mL | |
| 5 mM | 0.6912 mL | 3.4558 mL | 6.9116 mL | |
| 10 mM | 0.3456 mL | 1.7279 mL | 3.4558 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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