Lycoramine
Based on 1 Customer Validation
Lycoramine is a blood-brain barrier-penetrating Acetylcholinesterase inhibitor and Galanthamine (HY-76299) derivative. Lycoramine induces Amyloid-beta plaque clearance. Lycoramine induces reversal of cognitive decline and memory improvement. Lycoramine can be used for research on Alzheimer's disease and myasthenia gravis.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 99.83%
- CAS No.: 21133-52-8
- Formule: C17H23NO3
- Masse moléculaire:289.38
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Stockage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[3]|
AChE |
In Vitro
Lycoramine produces weaker AChE inhibition than Galanthamine (HY-76299) in the HPLC-IMER-MS bioanalytical system[1].
Lycoramine exhibits 42% higher acetylcholinesterase inhibitory activity than galantamine under in vitro conditions[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:5xFAD transgenic mice (12 month-old, sex equally distributed across groups, over-expressing APP with K670N, M671L, V717I mutations and PS1 with M146L and L286V mutations)[3]
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Dosage:4 mg/kg
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Administration:i.p.; daily; 7 days
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Result:Decreased escape latency in the acquisition phase of the Morris water maze test.
Increased time spent in the target quadrant during the probe phase.
Detected in all dissected brain regions (cortex, cerebellum, hippocampus, and remaining regions), confirming blood-brain barrier passage.
Caused a dramatic decrease in Aβ load, greater than galantamine.
Identified 2556 proteins in the cortex, with 145 proteins showing significant changes (fold change ≥ 1.3; q < 0.05).
Decreased cortical protein levels of clusterin (fc = 0.71, q = 0.00), apolipoprotein E (fc = 0.74, q = 0.009), microtubule-associated protein tau (fc = 0.49, q < 0.000), MAP1A (fc = 0.69, q < 0.000), MAP2 (fc = 0.44, q < 0.000), α-synuclein (fc = 0.49, q < 0.000), Tppp/25 (fc = 0.63, q < 0.000), GFAP (fc = 0.69, q = 0.004), Gja-1 (fc = 0.6, q = 0.007), AK-1 (fc = 0.67, q = 0.002), EHD3 (fc = 0.75, q = 0.019), and Synaptotagmin-5 (fc = 0.44, q = 0.006).
Increased cortical protein levels of GABRB2 (fc = 1.3, q = 0.011), Neurobeachin (fc = 1.3, q = 0.006), heat shock 70 kDa protein 1-like (fc = 1.35, q < 0.000), AT2B4/PMCA4 (fc = 1.81, q = 0.001), OSBP-1 (fc = 1.37, q = 0.018), and SRBS-1 (fc = 1.9, q = 0.004).
Increased cortical protein levels of Vimentin (fc = 1.43) and Gap junction alpha-1 protein (fc = 1.68).
Chemical Information
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CAS No. 21133-52-8
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Appearance Solid
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Masse moléculaire 289.38
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Formule C17H23NO3
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Color White to off-white
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SMILES
O[C@H]1CC[C@]23C4=C(O[C@]3(C1)[H])C(OC)=CC=C4CN(CC2)C
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Structure Classification
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Initial Source
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (345.57 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.64 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.64 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
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Protocol for Pharmacokinetic Study
Pharmacokinetic studies quantify how an organism handles a drug over time through absorption, distribution, metabolism, and excretion, and the core experimental readout is the concentration-time profile of parent drug and, when relevant, metabolites in biological matrices such as plasma, whole blood, urine, bile, or tissue. Pharmacokinetic analysis links dose, route, exposure, clearance, half-life, distribution, bioavailability, and systemic exposure to drug efficacy and toxicity hypotheses rather than measuring a signaling pathway directly. The literature links pharmacokinetics to drug-development phenotypes by showing that drug metabolism and pharmacokinetics influence compound progression, exposure-response interpretation, safety margins, dosing strategy, and failure risk during discovery and development. DMPK science contributes to compound optimization by integrating physicochemical properties, in vitro metabolism, transporter behavior, in vivo exposure, and pharmacodynamic contex
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Amyloid: Congo Red Amyloid Staining
Congo red amyloid staining is a histochemical method used to detect extracellular amyloid deposits in tissue sections based on the affinity of Congo red dye for β-pleated sheet-rich protein aggregates. When bound to amyloid, Congo red produces characteristic apple-green birefringence under polarized light microscopy, which is widely regarded as a diagnostic feature of amyloid deposition in histopathology. The diagnostic principle relies on the combination of dye binding (congophilia) and optical anisotropy under polarized illumination, which distinguishes amyloid from most non-amyloid eosinophilic extracellular deposits in routine histological evaluation. Amyloid identification by Congo red staining remains a cornerstone in diagnostic pathology despite the availability of adjunct methods such as immunohistochemistry and mass spectrometry, particularly because of its ability to localize deposits directly within tissue architecture. The specificity of Congo red-positive deposits is incre
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Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
Pureté et documentation
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Fiche technique (292 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1].
Yuan Y, et al. Online acetylcholinesterase inhibition evaluation by high-performance liquid chromatography-mass spectrometry hyphenated with an immobilized enzyme reactor. J Chromatogr A. 2020 Jan 4;1609:460506.
[Content Brief]
[2]. IRWIN RL, et al. Cholinesterase inhibition by galanthamine and lycoramine. Biochem Pharmacol. 1960 May;3:147-8. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.4557 mL | 17.2783 mL | 34.5566 mL | 86.3916 mL |
| 5 mM | 0.6911 mL | 3.4557 mL | 6.9113 mL | 17.2783 mL | |
| 10 mM | 0.3456 mL | 1.7278 mL | 3.4557 mL | 8.6392 mL | |
| 15 mM | 0.2304 mL | 1.1519 mL | 2.3038 mL | 5.7594 mL | |
| 20 mM | 0.1728 mL | 0.8639 mL | 1.7278 mL | 4.3196 mL | |
| 25 mM | 0.1382 mL | 0.6911 mL | 1.3823 mL | 3.4557 mL | |
| 30 mM | 0.1152 mL | 0.5759 mL | 1.1519 mL | 2.8797 mL | |
| 40 mM | 0.0864 mL | 0.4320 mL | 0.8639 mL | 2.1598 mL | |
| 50 mM | 0.0691 mL | 0.3456 mL | 0.6911 mL | 1.7278 mL | |
| 60 mM | 0.0576 mL | 0.2880 mL | 0.5759 mL | 1.4399 mL | |
| 80 mM | 0.0432 mL | 0.2160 mL | 0.4320 mL | 1.0799 mL | |
| 100 mM | 0.0346 mL | 0.1728 mL | 0.3456 mL | 0.8639 mL |
Lycoramine Related Classifications
HY-N6619A Related Classifications
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