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Galanthaminone {[allProObj[0].p_purity_real_show]}

货号:A258353 同义名: Narwedin;(-)-Narwedine

Galantamine is a competitive and reversible cholinesterase (AChE) inhibitor and is used for the treatment of mild to moderate Alzheimer's disease and various other memory impairments.

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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Galanthaminone 化学结构 CAS号:510-77-0
Galanthaminone 化学结构
CAS号:510-77-0
Galanthaminone 3D分子结构
CAS号:510-77-0
Galanthaminone 化学结构 CAS号:510-77-0
Galanthaminone 3D分子结构 CAS号:510-77-0
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Galanthaminone 纯度/质量文件 产品仅供科研

货号:A258353 标准纯度: {[allProObj[0].p_purity_real_show]}
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Galanthaminone 生物活性

描述 Galanthaminone (GAL) is a competitive and reversible cholinesterase (AChE) inhibitor; is used for the treatment of mild to moderate Alzheimer's disease and various other memory impairments[3]. The inhibition of acetylcholinesterase activity was closely correlated with the pharmacokinetics of galanthamine, a median maximal value of 53% being achieved by applying 10 mg galanthamine intravenously. Analysis of in vitro and ex vivo concentration responses revealed no differences, indicating that no metabolites of galanthamine exert additional inhibition of acetylcholinesterase activity[4]. In vivo, the maximal 36-55% inhibition of AChE was approached 30 min after oral administration of 10 mg GAL. The duration of the catalytic inhibition corresponded to an elimination half-life of approximately 5-7 h[5]. Galanthamine plasma peaks (1.24 micrograms/ml after subcutaneous and 1.15 micrograms/ml after oral doses) were reached 2 h following administration, the t1/2(beta) values being 5.70 and 5.26 h, respectively. An almost complete urinary recovery of galanthamine and its metabolites was obtained within 72 h. The plasma AUC, Cmax, tmax and ka suggest that the subcutaneous and oral Nivalin formulations are bioequivalent[6].

Galanthaminone 参考文献

[1]Heinrich M, Lee Teoh H. Galanthamine from snowdrop--the development of a modern drug against Alzheimer's disease from local Caucasian knowledge. J Ethnopharmacol. 2004 Jun;92(2-3):147-62.

[2]Greenblatt HM, Kryger G, et al. Structure of acetylcholinesterase complexed with (-)-galanthamine at 2.3 A resolution. FEBS Lett. 1999 Dec 17;463(3):321-6.

[3]Greenblatt HM, Kryger G, Lewis T, Silman I, Sussman JL. Structure of acetylcholinesterase complexed with (-)-galanthamine at 2.3 A resolution. FEBS Lett. 1999 Dec 17;463(3):321-6

[4]Bickel U, Thomsen T, Weber W, Fischer JP, Bachus R, Nitz M, Kewitz H. Pharmacokinetics of galanthamine in humans and corresponding cholinesterase inhibition. Clin Pharmacol Ther. 1991 Oct;50(4):420-8

[5]Thomsen T, Bickel U, Fischer JP, Kewitz H. Stereoselectivity of cholinesterase inhibition by galanthamine and tolerance in humans. Eur J Clin Pharmacol. 1990;39(6):603-5

[6]Mihailova D, Yamboliev I, Zhivkova Z, Tencheva J, Jovovich V. Pharmacokinetics of galanthamine hydrobromide after single subcutaneous and oral dosage in humans. Pharmacology. 1989;39(1):50-8

Galanthaminone 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.50mL

0.70mL

0.35mL

17.52mL

3.50mL

1.75mL

35.05mL

7.01mL

3.50mL

Galanthaminone 技术信息

CAS号510-77-0
分子式C17H19NO3
分子量 285.338
别名 Narwedin;(-)-Narwedine;3-Deoxy-3-oxo-galanthamine;Narwedine
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

溶解度

DMSO: 9 mg/mL(31.54 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

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