中文名稱:(-)-Huperzine A | 英文名稱:(-)-Huperzine A |
CAS:102518-79-6 | 品牌: 一研 |
保存條件: Store at -20°C | 產(chǎn)品類別: 抑制劑 |
Cas : 102518-79-6 |
產(chǎn)品屬性:
產(chǎn)品名稱 | 規(guī)格 | CAS號(hào) | 型號(hào) |
(-)-Huperzine A | 10mM (in 1mL DMSO) 10mg 25mg | 102518-79-6 | EY-Y0165053 |
Cas No.102518-79-6
別名 Huperzine A,
化學(xué)名 (5R,9R,E)-5-amino-11-ethylidene-7-methyl-5,6,9,10-tetrahydro-5,9-methanocycloocta[b]pyridin-2(1H)-one
分子式 C15H18N2O
分子量 242.3
溶解度 ≥ 12.1mg/mL in DMSO
儲(chǔ)存條件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產(chǎn)品描述:
(?)-Huperzine A (HupA) is an acetylcholinesterase (AChE) inhibitor with an IC50 value of 82 nmol/L [1] and acts as an antagonist of the N-methyl-d-aspartate (NMDA) receptor [2].
AChE is the key brain enzyme responsible for the rapid degradation of the neurotransmitter acetylcholine. AChE inhibitors are probably useful in the amelioration of the Alzheimer’s symptomatology [3].
It was found that NMDA markedly reduced AChE activities [4]. In rat dissociated hippocampal neurons, HupA inhibited the NMDA-induced current. In neurons, 100 μM HupA, NMDA-induced currents were 55.7 ± 4.9% of the control values. The binding molecular ratio of NMDA receptor: HupA is 1:1. The inhibition of NMDA receptor by HupA is not competitive [5]. HupA significantly increased the phosphorylation levels of both glycogen synthase kinase (GSK)-3α protein and GSK-3β protein in APPsw-overexpressing cells [2]. Activated GSK-3 consequently decreased acetylcholine (ACh) level in the striatum [6].
Treated with doses of (?)-huperzine A, AChE?/? mice showed no toxic symptoms and had normal levels of AChE. This demonstrated the specificity of (?)-huperzine A as an inhibitor of AChE at the dose used in vivo [7]. In rat whole brain, oral administration of HupA at a dose of 1.5 μmol/kg (3.6 mg/kg) obtained a maximum inhibition of AChE at 60 min and this maximum inhibition was maintained for 360 min [8].
References:
[1]. MA Xiao-Chao, XIN Jian, WANG Hai-Xue, et al. Acute effects of huperzine A and tacrine on rat liver. Acta Pharmacol ogica Sinica, 2003, 24(3):247-250.
[2]. Zhong Ming Qian and Ya Ke. Huperzine A: is it an effective disease-modifying drug for Alzheimer's disease? Frontiers in Aging Neuroscience, 2014, 6:216.
[3]. V. Rajendran, Suo-Bao Rong, Ashima Saxena, et al. Synthesis of a hybrid analog of the acetylcholinesterase inhibitors huperzine A and huperzine B. Tetrahedron Letters, 2001, 42: 5359-5361.
[4]. J. R. Delfs, D. M. Saroff, Y. Nishida, et al. Effects of NMDA and its antagonists on ventral horn cholinergic neurons in organotypic roller tube spinal cord cultures. J. Neural Transm., 1997, 104(1):31-51.
[5]. J. M. Zhang and G. Y. Hu. Huperzine A, a nootropic alkaloid, inhibits N-methyl-D-aspartate-induced current in rat dissociated hippocampal neurons. Neuroscience, 2001, 105(3):663-9.
[6]. L. Zhao, C. B. Chu, J. F. Li, et al. Glycogen synthase kinase-3 reduces acetylcholine level in striatum via disturbing cellular distribution of choline acetyltransferase in cholinergic interneurons in rats. Neuroscience, 2013, 255:203-11.
[7]. Ellen G. Duysen, Bin Li, Sultan Darvesh, et al. Sensitivity of butyrylcholinesterase knockout mice to (?)-huperzine A and donepezil suggests humans with butyrylcholinesterase deficiency may not tolerate these Alzheimer’s disease drugs and indicates butyrylcholinesterase function in neurotransmission. Toxicology, 2007, 233:60-69.
[8]. Rui Wang, Han Yan and Xi-can Tang. Progress in studies of huperzine A, a natural cholinesterase inhibitor from Chinese herbal medicine. Acta Pharmacologica Sinica, 2006, 27:1-26.
成立日期 | 2014-06-05 (11年) | 注冊資本 | 100 |
員工人數(shù) | 50-100人 | 年?duì)I業(yè)額 | ¥ 100萬以內(nèi) |
主營行業(yè) | 生化試劑,抗體,細(xì)胞培養(yǎng),分子生物學(xué),免疫安全 | 經(jīng)營模式 | 工廠,試劑 |
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