1. Neuronal Signaling
  2. AChE

Galanthamine (Synonyms: Galantamine)

Cat. No.: HY-76299 Purity: 99.78%
Data Sheet SDS Handling Instructions

Galanthamine is a potent acetylcholinesterase (AChE) inhibitor with IC50 of 500 nM.

For research use only. We do not sell to patients.
Galanthamine Chemical Structure

Galanthamine Chemical Structure

CAS No. : 357-70-0

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10 mM * 1 mL in DMSO $55 In-stock
50 mg $50 In-stock
100 mg $80 In-stock
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Other Forms of Galanthamine:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Galanthamine is a potent acetylcholinesterase (AChE) inhibitor with IC50 of 500 nM.

IC50 & Target

IC50: 0.5 μM (AChE)[1]

In Vitro

Galanthamine inhibits AChE and BChE with IC50 of 0.5 and 8.5 μM[1]. Galanthamine acts as a positive allosteric modulator (PAM) of human α4β2 AChRs expressed in permanently transfected HEK 293 cells. Galanthamine increases the response of (α4β2)2α5 AChRs to 1 μM ACh by up to 220% with very low concerntration(EC50=0.25 nM). Only small potentiation (20%) of either α4β2 or (α4β2)2β3 AChRs is detected using FLEXstation assays. Galanthamine at concentrations of 1 μM and above inhibits all three AChR subtypes[2].

In Vivo

Acute administration of Galantamine (0.3-3 mg/kg, i.p.) increases IGF2 mRNA levels in the hippocampus, but not in the prefrontal cortex, in time- and dose-dependent manner. Galantamine (3 mg/kg, i.p.) causes a transient increase in fibroblast growth factor 2 mRNA levels and a decrease in brain-derived neurotrophic factor mRNA levels in the hippocampus, while it does not affect the mRNA levels of other neurotrophic/growth factors. The Galantamine-induced increase in the hippocampal IGF2 mRNA levels is blocked by Mecamylamine, a nonselective nicotinic acetylcholine (ACh) receptor (nAChR) antagonist, and Methyllycaconitine, a selective α7 nAChR antagonist, but not by Telenzepine, a preferential M1muscarinic ACh receptor antagonist. Moreover, the selective α7 nAChR agonist PHA-543613 increasea the IGF2 mRNA levels, while Donepezil, an acetylcholinesterase inhibitor, does not. Galantamine also increases hippocampal IGF2 protein, which is blocked by Methyllycaconitine[2].

Clinical Trial
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References
Preparing Stock Solutions
Concentration Volume Mass 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
Please refer to the solubility information to select the appropriate solvent.
Animal Administration
[2]

Galanthamine is dissolved in saline (0.9 % solution of NaCl) (Mice)[2].

Mice[2]
Eight-week-old male ddY mice are housed in cages (24 cm×17 cm×12 cm) in each group of five to six animals under controlled environmental conditions (22±1°C; 12:12-h light-dark cycle, lights on at 0800 hours, food and water ad libitum) for 1 week before use in the experiments. 453 mice are used in total and in single use for each purpose. The following drugs are used: mecamylamine, methyllycaconitine, oxotremorine, and telenzepine, and Galantamine, Donepezil, and PHA-543613. All drugs are dissolved in saline (0.9 % solution of NaCl). Drugs are administered in a volume of 10 mL/kg intraperitoneally (i.p.) (Galantamine, Donepezil, Mecamylamine, Methyllycaconitine, Oxotremorine) or subcutaneously (s.c.) (PHA-543613, Telenzepine). MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

287.35

Formula

C₁₇H₂₁NO₃

CAS No.

357-70-0

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 59 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.78%

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Galanthamine
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HY-76299
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