| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
AChE[1]
O-Desmethyl Galanthamine targets acetylcholinesterase (AChE), acting as an inhibitor (antagonist). It has an IC50 of 1.83 μM for AChE inhibition. As a metabolite of galanthamine, it contributes to the overall pharmacological profile of the parent compound. |
|---|---|
| ln Vitro |
In cell-free enzyme assays, O-Desmethyl Galanthamine inhibits AChE activity with an IC50 of 1.83 μM. The compound is a galanthamine-type alkaloid and exhibits potent inhibitory activity against the enzyme, making it a valuable tool for studying cholinesterase inhibition. Cellular assays for O-Desmethyl Galanthamine are not extensively detailed in the available literature. However, as an AChE inhibitor, it would be expected to increase acetylcholine levels in neuronal cell cultures. Its activity can be assessed in cells expressing AChE by measuring the accumulation of acetylcholine.
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| ln Vivo |
In vivo, O-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 O-Desmethyl Galanthamine are performed using purified AChE enzyme. The enzyme is incubated with varying concentrations of the compound and a chromogenic substrate, such as acetylthiocholine. 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 O-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 O-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
Known metabolites of O-desmethylgalantamine include (2S,3S,4S,5R)-3,4,5-trihydroxy-6-[[(1S,12S,14R)-14-hydroxy-4-methyl-11-oxa-4-azatetracyclo[8.6.1.01,12.06,17]heptadec-6(17),7,9,15-tetraen-9-yl]oxy]oxacycloalkane-2-carboxylic acid and [(1S,12S,14R)-14-hydroxy-4-methyl-11-oxa-4-azatetracyclo[8.6.1.01,12.06,17]heptadec-6(17),7,9,15-tetraen-9-yl]hydrosulfate. O-desmethylgalantamine is a known metabolite of the human metabolite galantamine. The pharmacokinetic properties of O-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 O-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 |
Sanguinine is a benzo[a]azine. It has been reported in Lycoris radiata, Phaeranassa dubia, and other organisms with available data.
O-Desmethyl Galanthamine is a research compound used in Alzheimer's disease research. It is a galanthamine-type alkaloid and an AChE inhibitor. 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
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| Exact Mass |
273.136
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| CAS # |
60755-80-8
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| PubChem CID |
443722
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| Appearance |
White to off-white solid powder
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| Density |
1.37g/cm3
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| Boiling Point |
451.9ºC at 760 mmHg
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| Melting Point |
227-230ºC (dec.)
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| Flash Point |
227.1ºC
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| Index of Refraction |
1.683
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| LogP |
1.485
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
20
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| Complexity |
426
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| Defined Atom Stereocenter Count |
3
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| SMILES |
CN1CC[C@@]23C=C[C@@H](C[C@@H]2OC4=C(C=CC(=C34)C1)O)O
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| InChi Key |
OYSGWKOGUVOGFQ-RBOXIYTFSA-N
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| InChi Code |
InChI=1S/C16H19NO3/c1-17-7-6-16-5-4-11(18)8-13(16)20-15-12(19)3-2-10(9-17)14(15)16/h2-5,11,13,18-19H,6-9H2,1H3/t11-,13-,16-/m0/s1
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| Chemical Name |
(1S,12S,14R)-4-methyl-11-oxa-4-azatetracyclo[8.6.1.01,12.06,17]heptadeca-6(17),7,9,15-tetraene-9,14-diol
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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: 100 mg/mL (365.86 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.15 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 (9.15 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 (9.15 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 | 3.6586 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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