(-)-Huperzine A (Huperzine A) 是从Huperzia serrata分离得到的生物碱,具有神经保护活性。(-)-Huperzine A 是一种高效、高特异性、可逆的,具有血脑屏障渗透性的乙酰胆碱酯酶 (AChE) 抑制剂, 其IC50值为 82 nM。 (-)-Huperzine A 也是 N-甲基-D-天冬氨酸 (NMDA) 受体的非竞争性拮抗剂。(-)-Huperzine A 被开发用于神经退行性疾病的研究,包括阿尔茨海默病。
生物活性 | (-)-Huperzine A (Huperzine A) is an alkaloid isolated fromHuperzia serrata, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor ofacetylcholinesterase (AChE), with anIC50of 82 nM. (-)-Huperzine A also is non-competitive antagonist ofN-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease[1][2][3][4][5]. |
IC50& Target | |
体外研究 (In Vitro) | (-)-Huperzine A (1 μM; 2 hours) attenuates Aβ23-35 (20 μM)-induced neuronal injury[2]. (-)-Huperzine A (100 μM) reversibly inhibits the NMDA-induced current (IC50=126 μM) in whole-cell voltage-clamp recording in CA1 pyramidal neurons acutely dissociated from rat hippocampus[3].
|
体内研究 (In Vivo) | (-)-Huperzine A (0.1-0.2 mg/kg; i.p.; daily; for 12 days) can alleviate the cognitive dysfunction and neuronal degeneration induced by i.c.v. infusion of beta-amyloid protein-(1-40) in rats[5].
Animal Model: | Male Sprague-Dawley rats (220-280 g)[5] | Dosage: | 0.1 mg/kg, 0.2 mg/kg | Administration: | Intraperitoneal injection, daily, for 12 days | Result: | Partly reversed the down-regulation of anti-apoptotic Bcl-2 and the up-regulation of pro-apoptotic Bax and P53 proteins and reduced the apoptosis that normally followed b-amyloid injection; alleviated the cognitive dysfunction induced by b-amyloid protein-(1-40). |
|
Clinical Trial | |
分子量 | |
性状 | |
Formula | |
CAS 号 | |
中文名称 | |
结构分类 | - Alkaloids
- Pyridine Alkaloids
|
来源 | - Plants
- Huperziaceae
- Huperzia serrata
|
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
|
溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(412.68 mM) *"≥" means soluble, but saturation unknown. 配制储备液 1 mM | 4.1268 mL | 20.6339 mL | 41.2677 mL | 5 mM | 0.8254 mL | 4.1268 mL | 8.2535 mL | 10 mM | 0.4127 mL | 2.0634 mL | 4.1268 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro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,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制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 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (10.32 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (10.32 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (10.32 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (10.32 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (10.32 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (10.32 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
|