Size | Price | Stock | Qty |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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Other Sizes |
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Galanthamine is a potent and long-acting AChE inhibitor with IC50 of 0.35 μM, it exhibits 50-fold selectivity against butyryl-cholinesterase. It is a long-acting, centrally active acetylcholinesterase inhibitor and allosteric potentiator at neuronal nicotinic ACh receptors. It can prevents β-amyloid-induced apoptosis in SH-SY5Y and bovine chromaffin cells.
ln Vitro |
AChE and BChE are inhibited by galantamine, having IC50 values of 0.5 and 8.5 μM, respectively[1]. In permanently transfected HEK 293 cells, galantamine functions as a positive allosteric modulator (PAM) of human α4β2 AChR expression. At very low concentrations (EC50=0.25 nM), galantamine boosts the response of (α4β2)2α5 AChR to 1 μM ACh by up to 220%. Using the FLEXstation assay, only a minor increase (20%) of α4β2 or (α4β2)2β3 AChR was found. At concentrations greater than 1 μM, galantamine inhibits each of the three AChR subtypes [2].
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ln Vivo |
In the hippocampus, but not in the prefrontal cortex, acute galantamine administration (0.3–3 mg/kg, i.p.) raises IGF2 mRNA levels in a dose- and time-dependent manner. In the hippocampus, galantamine (3 mg/kg, i.p.) temporarily raises the mRNA levels of fibroblast growth factor 2 and decreases the mRNA levels of brain-derived neurotrophic factor, but has no effect on other neurotrophic/growth factors. mRNA concentrations. Mecamylamine, a nonselective nicotinic acetylcholine receptor (nAChR) antagonist, and methylaconitine, a selective α7 nAChR antagonist, can both suppress galantamine-induced increases in hippocampal IGF2 mRNA levels, but tirenzepine, a preferential M1 muscarinic ACh receptor antagonist, cannot. Additionally, IGF2 mRNA levels were elevated by the selective α7 nAChR agonist PHA-543613, but not by the acetylcholinesterase inhibitor donepezil. Additionally, methylaconitine can inhibit the rise of hippocampus IGF2 protein caused by galantamine [2].
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References |
[1]. Melanie-Jayne R. Howes, et al. Acetylcholinesterase inhibitors of natural origin. International Journal of Research in Pharmaceutical and Biomedical Sciences 3(SI 1):67-86.
[2]. Kuryatov A, et al. Roles of accessory subunits in alpha4beta2(*) nicotinic receptors. Mol Pharmacol. 2008 Jul;74(1):132-43. [3]. Kita Y, et al. Galantamine increases hippocampal insulin-like growth factor 2 expression via α7 nicotinic acetylcholine receptors in mice. Psychopharmacology (Berl). 2013 Feb;225(3):543-51 |
Molecular Formula |
C17H21NO3
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Molecular Weight |
287.3535
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CAS # |
357-70-0
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Related CAS # |
Galanthamine hydrobromide;1953-04-4;Galanthamine-d6;1128109-00-1;Galanthamine-O-methyl-d3;1279031-09-2
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O1C2=C(C([H])=C([H])C3C([H])([H])N(C([H])([H])[H])C([H])([H])C([H])([H])[C@]4(C([H])=C([H])[C@@]([H])(C([H])([H])[C@]14[H])O[H])C2=3)OC([H])([H])[H]
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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 : ≥ 59 mg/mL (~205.32 mM)
1M HCl : 50 mg/mL (~174.00 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.70 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 (8.70 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 (8.70 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 | 3.4801 mL | 17.4004 mL | 34.8008 mL | |
5 mM | 0.6960 mL | 3.4801 mL | 6.9602 mL | |
10 mM | 0.3480 mL | 1.7400 mL | 3.4801 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.