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

Galanthamine  (Synonyms: 加蘭他敏; Galantamine)

目錄號: HY-76299 純度: 99.96%
COA 產(chǎn)品使用指南 技術(shù)支持

Galanthamine 是一種有效的乙酰膽堿酯酶 (AChE) 抑制劑，IC50 為 500 nM。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

Galanthamine Chemical Structure

Galanthamine Chemical Structure

CAS No. : 357-70-0

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3.  試用裝只面向終端客戶。

規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥605
In-stock
50 mg ￥550
In-stock
100 mg ￥850
In-stock
200 mg   詢價(jià)  
500 mg   詢價(jià)  

* Please select Quantity before adding items.

Customer Review

Other Forms of Galanthamine:

查看 Cholinesterase (ChE) 亞型特異性產(chǎn)品:

  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

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

IC50 & Target

AChE

 

細(xì)胞效力
(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]
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]
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
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]
體外研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量

287.35

Formula

C17H21NO3
CAS 號
性狀

固體

顏色

White to off-white

中文名稱

加蘭他敏；加蘭他明；尼瓦林；強(qiáng)??；雪花胺；雪花蓮胺
結(jié)構(gòu)分類
初始來源
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : ≥ 59 mg/mL (205.32 mM; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制儲備液
濃度 溶劑體積 質(zhì)量 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
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時(shí)，請?jiān)?年內(nèi)使用， -20°C儲存時(shí)，請?jiān)?年內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn)：

請根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (8.70 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

    2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
  • 方案 二

    請依序添加每種溶劑： 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (8.70 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液，此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL玉米油中，混合均勻。

動(dòng)物溶解方案計(jì)算器
請輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
請輸入您的動(dòng)物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
您所需的儲備液濃度超過該產(chǎn)品的實(shí)測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過半月以上，請謹(jǐn)慎選擇該方案。
請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.96%

參考文獻(xiàn)
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 has not independently confirmed the accuracy of these methods. They are for reference only.
參考文獻(xiàn)

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時(shí)，請?jiān)?年內(nèi)使用， -20°C儲存時(shí)，請?jiān)?年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.4801 mL 17.4004 mL 34.8008 mL 87.0019 mL
5 mM 0.6960 mL 3.4801 mL 6.9602 mL 17.4004 mL
10 mM 0.3480 mL 1.7400 mL 3.4801 mL 8.7002 mL
15 mM 0.2320 mL 1.1600 mL 2.3201 mL 5.8001 mL
20 mM 0.1740 mL 0.8700 mL 1.7400 mL 4.3501 mL
25 mM 0.1392 mL 0.6960 mL 1.3920 mL 3.4801 mL
30 mM 0.1160 mL 0.5800 mL 1.1600 mL 2.9001 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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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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產(chǎn)品名稱：
Galanthamine
目錄號：
HY-76299
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