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(-)-Huperzine A

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Chemical Structure| 102518-79-6 同义名 : 石杉碱 ;Hup A;(−)-Selagine;(-)-Selagine.;Selagine;(−)-Huperzine A;Huperzine A
CAS号 : 102518-79-6
货号 : A161814
分子式 : C15H18N2O
纯度 : 98%
分子量 : 242.316
MDL号 : MFCD01714949
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(433.32 mM)，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
动物实验配方：

30% propylene glycol+5% Tween 80+65% water 30 mg/mL suspension

生物活性
靶点

  • AChE

    AChE (G4 form), Ki:7 nM

  • GluR

    AChE (G4 form), Ki:7 nM
描述 Huperzine A, an active Lycopodium alkaloid extracted from traditional Chinese herb, is a potent, reversible, selective inhibitor of acetylcholinesterase (AChE) used in China for the treatment of Alzheimer's disease[3]. Inhibition of fetal bovine serum acetylcholinesterase by (-)-Huperzine A was 35-fold more potent than (+)-Huperzine A, with KI values of 6.2 nM and 210 nM, respectively. In addition, (-)-Huperzine A was 88-fold more potent in inhibiting Torpedo acetylcholinesterase than (+)-Huperzine A, with KI values of 0.25 mM and 22 mM, respectively[4]. Huperzine A treatment significantly decreased the level of intracellular Aβ42 and ameliorated oligomeric Aβ42 induced mitochondrial dysfunctions in primary cortical neurons[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.13mL

0.83mL

0.41mL

20.63mL

4.13mL

2.06mL

41.27mL

8.25mL

4.13mL
参考文献

[1]Zhang HY, Tang XC. Neuroprotective effects of huperzine A: new therapeutic targets for neurodegenerative disease. Trends Pharmacol Sci. 2006 Dec;27(12):619-25.

[2]Zhao Q, Tang XC. Effects of huperzine A on acetylcholinesterase isoforms in vitro: comparison with tacrine, donepezil, rivastigmine and physostigmine. Eur J Pharmacol. 2002 Nov 29;455(2-3):101-7.

[3]Lei Y, Yang L, Ye CY, Qin MY, Yang HY, Jiang HL, Tang XC, Zhang HY. Involvement of Intracellular and Mitochondrial Aβ in the Ameliorative Effects of Huperzine A against Oligomeric Aβ42-Induced Injury in Primary Rat Neurons. PLoS One. 2015 May 29;10(5):e0128366.

[4]Saxena A, Qian N, Kovach IM, Kozikowski AP, Pang YP, Vellom DC, Radić Z, Quinn D, Taylor P, Doctor BP. Identification of amino acid residues involved in the binding of Huperzine A to cholinesterases. Protein Sci. 1994 Oct;3(10):1770-8.

[5]Lei Y, Yang L, Ye CY, Qin MY, Yang HY, Jiang HL, Tang XC, Zhang HY. Involvement of Intracellular and Mitochondrial Aβ in the Ameliorative Effects of Huperzine A against Oligomeric Aβ42-Induced Injury in Primary Rat Neurons. PLoS One. 2015 May 29;10(5):e0128366.