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(-)-Huperzine A/石杉碱甲 {[allProObj[0].p_purity_real_show]}

货号:A161814 同义名: 石杉碱 / Hup A; (-)-Selagine.

(-)-Huperzine A是一种天然存在的龙脑类生物碱,能抑制乙酰胆碱酯酶(AChE)。

HazMat Fee +

There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

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+
(-)-Huperzine A/石杉碱甲 化学结构 CAS号:102518-79-6
(-)-Huperzine A/石杉碱甲 化学结构
CAS号:102518-79-6
(-)-Huperzine A/石杉碱甲 3D分子结构
CAS号:102518-79-6
(-)-Huperzine A/石杉碱甲 化学结构 CAS号:102518-79-6
(-)-Huperzine A/石杉碱甲 3D分子结构 CAS号:102518-79-6
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(-)-Huperzine A/石杉碱甲 纯度/质量文件 产品仅供科研

货号:A161814 标准纯度: {[allProObj[0].p_purity_real_show]}
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(-)-Huperzine A/石杉碱甲 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].

(-)-Huperzine A/石杉碱甲 细胞实验

Cell Line
Concentration Treated Time Description References
Rat cortical neurons 1 μM and 10 μM 24 h To evaluate the effects of HupA on iron overload-induced LIP level increase. Results showed that HupA significantly decreased the iron overload-induced LIP level increase. Acta Pharmacol Sin. 2016 Nov;37(11):1391-1400
Rat cortical neurons 1 μM and 10 μM 24 h To evaluate the effects of HupA on iron overload-induced ATP decrease. Results showed that HupA significantly ameliorated the iron overload-induced ATP decrease. Acta Pharmacol Sin. 2016 Nov;37(11):1391-1400
Rat cortical neurons 1 μM and 10 μM 24 h To evaluate the effects of HupA on iron overload-induced ROS formation. Results showed that HupA significantly inhibited the iron overload-induced increase in ROS. Acta Pharmacol Sin. 2016 Nov;37(11):1391-1400
Rat cortical neurons 1 μM and 10 μM 24 h To evaluate the protective effects of HupA against iron overload-induced neuronal damage. Results showed that HupA significantly attenuated the iron overload-induced decrease in neuronal cell viability and improved neuronal morphology. Acta Pharmacol Sin. 2016 Nov;37(11):1391-1400
SH-SY5Y cells 10 μM 24 h HupA significantly increased ADAM10 levels, decreased BACE1 levels, increased sAPPα and C83 fragments, and decreased sAPPβ and C99 fragments, indicating that HupA modulates APP processing by enhancing the nonamyloidogenic pathway. Neuropsychopharmacology. 2011 Apr;36(5):1073-89

(-)-Huperzine A/石杉碱甲 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice High-fat diet-induced obese mice and ob/ob mice Intragastric administration 0.1 mg/kg/day and 0.3 mg/kg/day Once daily for 3 months Hup A (0.1 mg/kg/day) improved both the abilities of object recognition and spatial memory in HFD-fed mice, but not in ob/ob mice. Furthermore, Hup A treatment significantly upregulated the insulin and phosphorylated Akt levels in the cortex of HFD-fed mice, but not ob/ob mice. In addition, Hup A (0.3 mg/kg/day) significantly decreased cortical β-secretase (BACE1) expression. Acta Pharmacol Sin. 2020 Feb;41(2):145-153
C57BL/6N mice Chronic intermittent hypoxia model Intraperitoneal injection 0.1 mg/kg/day Once daily for 21 days Huperzine A-Liposomes (HuA-LIP) significantly ameliorated cognitive dysfunction and neuronal damage in CIH mice, elevated T-SOD and GSH-Px abilities, decreased MDA content, reduced brain iron levels by downregulating TfR1, hepcidin, and FTL expression, and improved synaptic plasticity by activating the PKAα/Erk/CREB/BDNF signaling pathway and elevating MAP2, PSD95, and synaptophysin. Int J Nanomedicine. 2023 Feb 17;18:843-859
APP/PS1 double-transgenic mice Alzheimer's disease model Intranasal administration 167 and 500 μg/kg Once daily for 4 months HupA reduced Aβ burden and generation, enhanced nonamyloidogenic processing of APP by inhibiting GSK3α/β activity and enhancing β-catenin levels, suggesting its neuroprotective effects involve not only AChE inhibition and antioxidation but also modulation of the Wnt/β-catenin signaling pathway. Neuropsychopharmacology. 2011 Apr;36(5):1073-89

(-)-Huperzine A/石杉碱甲 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.

(-)-Huperzine A/石杉碱甲 实验方案

计算器
存储液制备 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

(-)-Huperzine A/石杉碱甲 技术信息

CAS号102518-79-6
分子式C15H18N2O
分子量 242.32
SMILES Code O=C1C=CC([C@@](/C2=C/C)(N)CC(C)=C[C@@]2([H])C3)=C3N1
MDL No. MFCD01714949
别名 石杉碱 ;Hup A; (-)-Selagine.; Selagine; Huperzine A
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C

溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三
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