| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
N-Desmethyl Galanthamine targets acetylcholinesterase (AChE) and cholinesterase (ChE). It is an EeAChE inhibitor with an IC50 of 2.76 μM. As a metabolite of galanthamine, it may contribute to the overall pharmacological effects of the parent compound, particularly in the context of Alzheimer's disease research.
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|---|---|
| ln Vitro |
In cell-free enzyme assays, N-Desmethyl Galanthamine inhibits AChE with an IC50 of 2.76 μM. It exhibits inhibitory activity against both AChE and ChE. These assays confirm its potency as a cholinesterase inhibitor, making it a valuable tool for studying Alzheimer's disease. Cellular assays for N-Desmethyl Galanthamine are not extensively detailed. However, as an AChE/ChE inhibitor, it would be expected to increase acetylcholine levels in neuronal cell cultures. Its activity can be assessed in cells expressing these enzymes by measuring the accumulation of acetylcholine.
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| ln Vivo |
In vivo, N-Desmethyl Galanthamine is a metabolite of galanthamine. It may contribute to the pharmacological effects of galanthamine, including its cognitive-enhancing properties. Studies on its specific in vivo effects are limited, but it is used in research on Alzheimer's disease.
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| Enzyme Assay |
Cell-free enzyme inhibition assays for N-Desmethyl Galanthamine are performed using purified AChE or ChE enzymes. The enzyme is incubated with varying concentrations of the compound and a chromogenic substrate. The rate of substrate hydrolysis is measured spectrophotometrically, and the IC50 value is determined from the inhibition curve.
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| Cell Assay |
Cellular assays for N-Desmethyl Galanthamine could be conducted using neuronal cell lines. Cells would be treated with the compound, and markers of cholinergic function, such as acetylcholine levels, could be measured. Neuroprotective effects could be assessed in models of neurodegeneration.
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| Animal Protocol |
In vivo studies on N-Desmethyl Galanthamine are limited, as it is primarily studied as a metabolite. It may be administered to animal models to study its pharmacokinetics and contribution to the effects of galanthamine. Its role in Alzheimer's disease research is of interest.
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| ADME/Pharmacokinetics |
Metabolism/Metabolites
N-Demethylgalantamine is a known metabolite of galantamine in the human body. The pharmacokinetic properties of N-Desmethyl Galanthamine are related to its role as a metabolite of galanthamine. It is formed in the body through demethylation of galanthamine. Its half-life and distribution would be influenced by its physicochemical properties. |
| Toxicity/Toxicokinetics |
Preclinical toxicity data for N-Desmethyl Galanthamine are limited. As a metabolite of a clinically used drug, its safety profile is likely similar to that of galanthamine. Comprehensive toxicological studies have been conducted for the parent compound.
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| References | |
| Additional Infomation |
Norgalanthamine is a benzodiazepine compound. It has been reported to exist in Snowdropa purpurea, Snowdropa elvis, and other organisms with relevant data.
N-Desmethyl Galanthamine is a research compound used in Alzheimer's disease research. It is a metabolite of galanthamine and exhibits inhibitory activity against AChE and ChE. Its role as a metabolite makes it a valuable tool for studying the metabolism and pharmacology of galanthamine. It is not approved for clinical use. |
| Molecular Formula |
C16H19NO3
|
|---|---|
| Molecular Weight |
273.33
|
| Exact Mass |
273.136
|
| CAS # |
41303-74-6
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| PubChem CID |
9838394
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| Appearance |
White to off-white solid powder
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| Density |
1.309g/cm3
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| Boiling Point |
457.923ºC at 760 mmHg
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| Melting Point |
142-145ºC
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| Flash Point |
230.744ºC
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| Index of Refraction |
1.642
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| LogP |
1.836
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
1
|
| Heavy Atom Count |
20
|
| Complexity |
413
|
| Defined Atom Stereocenter Count |
3
|
| SMILES |
COC1=C2C3=C(CNCC[C@]34C=C[C@@H](C[C@@H]4O2)O)C=C1
|
| InChi Key |
AIXQQSTVOSFSMO-RBOXIYTFSA-N
|
| InChi Code |
InChI=1S/C16H19NO3/c1-19-12-3-2-10-9-17-7-6-16-5-4-11(18)8-13(16)20-15(12)14(10)16/h2-5,11,13,17-18H,6-9H2,1H3/t11-,13-,16-/m0/s1
|
| Chemical Name |
(1S,12S,14R)-9-methoxy-11-oxa-4-azatetracyclo[8.6.1.01,12.06,17]heptadeca-6(17),7,9,15-tetraen-14-ol
|
| 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) |
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 | 3.6586 mL | 18.2929 mL | 36.5858 mL | |
| 5 mM | 0.7317 mL | 3.6586 mL | 7.3172 mL | |
| 10 mM | 0.3659 mL | 1.8293 mL | 3.6586 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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