1. Neuronal Signaling Apoptosis
  2. Cholinesterase (ChE) Apoptosis
  3. Galanthamine

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

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Galanthamine

Galanthamine 화학구조

CAS No. : 357-70-0

사이즈 가격 재고 수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
50 mg 해외재고보유
100 mg 해외재고보유
200 mg   견적 받기  
500 mg   견적 받기  

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 15 publication(s) in Google Scholar

Other Forms of Galanthamine:

Top Publications Citing Use of Products

View All Cholinesterase (ChE) Isoform Specific Products:

  • Biological Activity

  • Protocol

  • 순도&문서

  • References

  • 고객리뷰

제품 설명

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

IC50 & Target

AChE

 

Cellular Effect
Cell Line Type Value Description References
BJ IC50
> 50 μM
Compound: 1
Cytotoxicity against human BJ cells after 72 hrs by Calcein AM assay
Cytotoxicity against human BJ cells after 72 hrs by Calcein AM assay
[PMID: 22921081]
CCRF-CEM IC50
> 50 μM
Compound: 1
Cytotoxicity against human CEM cells after 72 hrs by Calcein AM assay
Cytotoxicity against human CEM cells after 72 hrs by Calcein AM assay
[PMID: 22921081]
Cortical neurone EC50
1.48 μM
Compound: Galantamine
Neuroprotective activity against NMDA-induced excitotoxicity in Sprague-Dawley rat primary cortical neurons assessed as increase in cell viability after 3 hrs by MTT assay
Neuroprotective activity against NMDA-induced excitotoxicity in Sprague-Dawley rat primary cortical neurons assessed as increase in cell viability after 3 hrs by MTT assay
[PMID: 27376495]
G-361 IC50
> 50 μM
Compound: 1
Cytotoxicity against human G361 cells after 72 hrs by Calcein AM assay
Cytotoxicity against human G361 cells after 72 hrs by Calcein AM assay
[PMID: 22921081]
HeLa IC50
> 50 μM
Compound: 1
Cytotoxicity against human HeLa cells after 72 hrs by Calcein AM assay
Cytotoxicity against human HeLa cells after 72 hrs by Calcein AM assay
[PMID: 22921081]
HepG2 IC50
4200 μM
Compound: Galantamine
Cytotoxicity against human HepG2 cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay
[PMID: 36996715]
HepG2 IC50
4200 μM
Compound: Galantamine
Cytotoxicity against human HepG2 cells incubated for 24 hrs by MTT assay
Cytotoxicity against human HepG2 cells incubated for 24 hrs by MTT assay
[PMID: 38784455]
K562 IC50
> 50 μM
Compound: 1
Cytotoxicity against human K562 cells after 72 hrs by Calcein AM assay
Cytotoxicity against human K562 cells after 72 hrs by Calcein AM assay
[PMID: 22921081]
MCF7 IC50
> 50 μM
Compound: 1
Cytotoxicity against human MCF7 cells after 72 hrs by Calcein AM assay
Cytotoxicity against human MCF7 cells after 72 hrs by Calcein AM assay
[PMID: 22921081]
NIH3T3 IC50
7.28 μM
Compound: Galanthamine
Cytotoxicity against mouse NIH/3T3 cells incubated for 24 hrs by MTT assay
Cytotoxicity against mouse NIH/3T3 cells incubated for 24 hrs by MTT assay
[PMID: 38614062]
SH-SY5Y EC50
1.94 μM
Compound: Galantamine
Neuroprotective activity against okadaic acid-induced tau phosphorylation-mediated cell death in human SH-SY5Y cells assessed as increase in cell viability after 24 hrs by XTT assay
Neuroprotective activity against okadaic acid-induced tau phosphorylation-mediated cell death in human SH-SY5Y cells assessed as increase in cell viability after 24 hrs by XTT assay
[PMID: 27376495]
SH-SY5Y EC50
2.81 μM
Compound: Galantamine
Neuroprotective activity against oligomycine/rotenone-induced oxidative stress-mediated cell death in human SH-SY5Y cells assessed as increase in cell viability after 24 hrs by XTT assay
Neuroprotective activity against oligomycine/rotenone-induced oxidative stress-mediated cell death in human SH-SY5Y cells assessed as increase in cell viability after 24 hrs by XTT assay
[PMID: 27376495]
SH-SY5Y IC50
4700 μM
Compound: Galantamine
Cytotoxicity against human SH-SY5Y cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay
Cytotoxicity against human SH-SY5Y cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay
[PMID: 36996715]
SH-SY5Y IC50
4700 μM
Compound: Galantamine
Cytotoxicity against human SH-SY5Y cells incubated for 24 hrs by MTT assay
Cytotoxicity against human SH-SY5Y cells incubated for 24 hrs by MTT assay
[PMID: 38784455]
SH-SY5Y IC50
747 nM
Compound: 1
Neuroprotective activity in human SH-SY5Y cells assessed as protection against NMDA-induced cell death after 6 hrs by MTS assay
Neuroprotective activity in human SH-SY5Y cells assessed as protection against NMDA-induced cell death after 6 hrs by MTS assay
[PMID: 23033965]
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
분자량

287.36

화학식

C17H21NO3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O[C@@H]1C[C@@H]2OC3=C4C(CN(C)CC[C@]42C=C1)=CC=C3OC

Structure Classification
Initial Source
선적

Room temperature in continental US; may vary elsewhere.

보관
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
용액&용해도
In Vitro: 

DMSO : ≥ 59 mg/mL (205.32 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4800 mL 17.3998 mL 34.7997 mL
5 mM 0.6960 mL 3.4800 mL 6.9599 mL
View the 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • 몰농도 계산기

  • 농도 희석 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (8.70 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (8.70 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
순도&문서

Purity: 99.90%

References
Animal Administration
[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 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.

References

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.4800 mL 17.3998 mL 34.7997 mL 86.9992 mL
5 mM 0.6960 mL 3.4800 mL 6.9599 mL 17.3998 mL
10 mM 0.3480 mL 1.7400 mL 3.4800 mL 8.6999 mL
15 mM 0.2320 mL 1.1600 mL 2.3200 mL 5.7999 mL
20 mM 0.1740 mL 0.8700 mL 1.7400 mL 4.3500 mL
25 mM 0.1392 mL 0.6960 mL 1.3920 mL 3.4800 mL
30 mM 0.1160 mL 0.5800 mL 1.1600 mL 2.9000 mL
40 mM 0.0870 mL 0.4350 mL 0.8700 mL 2.1750 mL
50 mM 0.0696 mL 0.3480 mL 0.6960 mL 1.7400 mL
60 mM 0.0580 mL 0.2900 mL 0.5800 mL 1.4500 mL
80 mM 0.0435 mL 0.2175 mL 0.4350 mL 1.0875 mL
100 mM 0.0348 mL 0.1740 mL 0.3480 mL 0.8700 mL
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상품명:
Galanthamine
Cat. No.:
HY-76299
수량:
MCE Japan Authorized Agent: