Galanthamine

別名:Galantamine, Nivalin, Razadyne, Razadyne ER, Reminyl, Lycoremine

Galanthamine (Galantamine, Nivalin, Razadyne, Razadyne ER, Reminyl, Lycoremine) is a phenanthrene alkaloid and a reversible, competitive acetylcholinesterase inhibitor with IC50 of 0.35 μM, exhibits 50-fold selectivity against butyryl-cholinesterase. It is studied as a treatment for Alzheimer's disease and other central nervous system disorders.

Galanthamine化学構造

CAS No. 357-70-0

サイズ 価格(税別) 在庫状況
JPY 15900 国内在庫あり
JPY 144600 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール:[email protected]
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文献中Selleckの製品使用例(1)

製品安全説明書

現在のバッチを見る: 純度: 99.97%
99.97

Galanthamine関連製品

シグナル伝達経路

AChR阻害剤の選択性比較

生物活性

製品説明 Galanthamine (Galantamine, Nivalin, Razadyne, Razadyne ER, Reminyl, Lycoremine) is a phenanthrene alkaloid and a reversible, competitive acetylcholinesterase inhibitor with IC50 of 0.35 μM, exhibits 50-fold selectivity against butyryl-cholinesterase. It is studied as a treatment for Alzheimer's disease and other central nervous system disorders.
Targets
AChE [1]
(Cell-free assay)
0.35 μM
In Vitro
In vitro Galantamine shows reversible, competitive acetylcholinesterase inhibiting and nicotinic acetylcholinergic receptor modulatory properties[2]. Galantamine reduced the release of reactive oxygen species (up to 50%) and prevented loss in mitochondrial activity. Galantamine treatment resulted in a significant inhibition of H2O2-induced nitrite generation. Galantamine also concentration-dependently inhibited AChE activity (28–88%) in H2O2–SK-N-SH cells after 24 h. This drug, which facilitates cholinergic neurotransmission, is also neuroprotective by lowering oxidative injury[3].
細胞実験 細胞株 SK-N-SH cells
濃度 0.1-100 μM
反応時間 24 h
実験の流れ Cells are seeded in 96-multiwell dishes at a density of 100,000 cells/ml (100 ml in each well) for cytotoxicity and fluorescence detection or in six-well dishes (1 ml in each well) for measuring NO production and acetylcholinesterase (AChE) activity. Cells are treated with the drugs in serum-free DMEM. Experiments are carried out 24–48 h after cells are seeded. Cells are exposed for 2 h, either to H2O2 (500 μM), or galantamine alone (0.1-100 μM), or to the combination of H2O2 plus galantamine. As no change in AChE activity is seen after 2 h, SK-N-SH cells are also incubated with galantamine for 24 h.
In Vivo
In Vivo Generally, oral absorption was rapid, with maximal plasma levels reached within 2 h in all species. Absolute oral bioavailability of a gavage dose was high in rat (77 %) and dog (78 %). In mice and rats, the bioavailability of galantamine administered via the food was lower than of galantamine administered by gavage. Elimination half-life of galantamine was relatively large in rat and dog and smaller in mouse and rabbit. After i.v. administration, galantamine plasma levels declined fairly rapidly in the various animal species tested with an elimination half-life of 1−5 h in the rat and 4−7 h in the dog. The volume of distribution was 4−5 l/kg in rats and dogs. Plasma clearance was highest in male rats, 1.9 l/kg/h, about twice the value of female rats and of dogs. Sex differences in pharmacokinetics of galantamine were shown to exist in rats and mice. Male rats generally had lower plasma values of galantamine and lower exposure rates; in mice, the effect was opposite. In dogs, no sex differences in the pharmacokinetics of galantamine could be detected. In mice and rats, the bioavailability of galantamine administered via the food was lower than of galantamine administered by gavage[2].
動物実験 動物モデル Male Sprague Dawley rats
投与量 0, 0.1, 1.0, or 5.0 mg/kg
投与経路 i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00299676 Completed
Alzheimer Disease|Dementia|Galantamine
Janssen-Cilag Pty Ltd
May 2005 --

化学情報

分子量 287.35 化学式

C17H21NO3

CAS No. 357-70-0 SDF --
保管

In vitro
Batch:

DMSO : 40 mg/mL ( (139.2 mM); 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : 20 mg/mL

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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